Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
Agonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assayAgonist activity at mouse H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by luciferase reporter gene assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation countingInhibition of basal activity of human histamine H3 receptor expressed in CHO cells assessed as inhibition of RAHM-induced [35S]GTPgammaS binding after 4 hrs by beta liquid scintillation counting
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to controlInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of RAMH-induced [35S]GTPgammaS binding relative to control
Inverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor (445 amino acid residues) expressed in CHO cells by CRE-luciferase reporter gene assay
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as decrease of basal activity of [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-LucAntagonist activity at human histamine H3 receptor expressed in CHO cells co-expressing CRE-Luc
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
In vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro intrinsic activity against histamine H3 receptor from synaptosomes of rat cerebral cortex
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 histamine receptor by [35S]GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]GTPgammaS binding assay
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Antagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assayAntagonist activity at human histamine H3 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human H3 receptor by [35S]GTPgamma binding assayInverse agonist activity at human H3 receptor by [35S]GTPgamma binding assay
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
Inverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by [35S]-GTPgammaS binding assay
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma bindingInverse agonist activity at human H3 receptor expressed in HEK293T cells assessed as inhibition of {35S]GTPgamma binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Agonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assayAgonist activity at recombinant human H3R expressed on cells incubated for 60 mins by [35S]GTPgammaS binding assay
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
The compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMThe compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
Antagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assayAntagonist activity at recombinant human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation after 30 mins by TR-FRET TR-FRET assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Agonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at human histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Antagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assayAntagonist activity at human histamine 3 receptor by [35S]GTPgammaS binding assay
Inverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human H3R expressed in CHO cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
Inverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS bindingInverse agonist activity at rat histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine induced [35S]GTPgammaS binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assay
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gsalpha2, Gbeta1gamma2 and RGS19 by steady-state GTPase activity assay
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgammaS assay
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, G-beta-1-gamma-2 and RGS4 by steady-state GTPase activity assay
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
Agonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assayAgonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayAgonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Antagonist activity at H3 receptor assessed as inhibition of [35S]gammaGTP binding relative to controlAntagonist activity at H3 receptor assessed as inhibition of [35S]gammaGTP binding relative to control
Agonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assayAgonist activity at human H3R expressed in HEK293T-SP-FLAG-hH3R-CRE-CBR cells incubated for 5 hrs by luciferase reporter gene assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Agonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assayAgonist activity at human H3 receptor stably transfected in CHO-DUKX cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level by HitHunter-cAMP assay
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor assessed as beta galactosidase activityAgonist activity at human histamine H3 receptor assessed as beta galactosidase activity
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activityAgonist activity at human histamine H3 receptor in SK-N-MC cells assessed as inhibition of forskolin-induced cAMP-mediated CRE-beta galactosidase activity
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Effective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cellsEffective concentration required against human histamine H3 receptor was determined by the inhibition of the cAMP stimulated beta-galactosidase transcription in SK-N-MC cells
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assayInverse agonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation by luciferase reporter gene assay
Agonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assayAgonist activity at human H3 receptor expressed in CHO cells assessed as increase in cAMP accumulation by measuring reduction in forskolin level incubated for 4 hrs by CRE/MRE-luciferase reporter gene assay
Compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
Compound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for agonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting methodAgonist activity at human H3 receptor expressed in HEK293 cells preincubated for 30 mins followed by [35S]-GTPgammaS addition and measured after 30 mins by liquid scintillation counting method
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assayAgonist activity at human H3R-Galphai2-Gbeta1gamma2-RGS4 expressed in Sf9 cells 0.1 nM to 1 mM by steady state GTPase activity assay
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
In vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortexIn vitro binding affinity against histamine H3 receptor from synaptosomes of rat cerebral cortex
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on SK-N-MC cells assessed as inhibition of forskolin-induced beta galactosidase activity preincubated with forskolin for 6 hrs followed compound addition by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Inverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma bindingInverse agonist activity at histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgamma binding
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assayActivity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai, Gbeta1gamma2 and RGS4 by steady-state GTPase activity assay
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Compound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uMCompound was evaluated for antagonistic effect on release of [3H]histamine from rat brain cortical slices with L-[3H]histidine at 0.3 uM
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assayAgonist activity at human H3R expressed on HEK293T cells by [35S]GTPgammaS binding assay
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Agonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S bindingAgonist activity at rat histamine H3 receptor expressed in HEK239 cells assessed as reduction of basal [35S]GTP-gamma-S binding
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
Agonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
Antagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassayAntagonist activity at human recombinant histamine H3 receptor expressed in HEK293 cells assessed as inhibition of forskolin/(R)(-)-alpha-methylhistamine-induced cAMP accumulation after 1 hr by TR-FRET immunoassay
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assayAgonist activity at human H3R expressed on HEK293T cells assessed as inhibition of forskolin-induced CRE-driven luciferase activity co-incubated with forskolin for 6 hrs and measured after 30 mins by CRE-luciferase reporter gene assay
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Agonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingAgonist activity at human histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptorInhibition of cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing human H3 receptor
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation countingInverse agonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of [35S]-GTPgammaS binding by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Agonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assayAgonist activity at human histamine H3 receptor expressed in human SK-N-MC cells by CRE-beta galactosidase reporter gene assay
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO-K1 cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Agonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assayAgonist activity at human H3 receptor expressed in 293-EBNA cells by luciferase reporter gene assay
Agonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assayAgonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assay
Agonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation countingAgonist activity at human recombinant histamine H3 receptor expressed in CHO cells assessed as [35S]GTPgammaS binding after 1 hr by liquid scintillation counting
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assayInverse agonist activity at human histamine H3 receptor expressed in CHO cells by GTPgamma[35S] binding assay
Inhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibitory activity determined by the inhibition of cAMP- stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Displacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cellsDisplacement of [125H]iodoproxyphan from human recombinant histamine H3 receptor expressed in human SK-N-MC cells
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Inhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptorInhibition of the cAMP-stimulated beta-galactosidase transcription in SK-N-MC cells expressing the human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Agonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assayAgonist activity at human H3R expressed in HEK293 cells harboring glosensor-22F cAMP plasmid DNA assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated with cells followed by forskolin addition measured after 10 mins by luminescence assay
Inverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS bindingInverse agonist activity at human recombinant histamine H3 receptor assessed as effect on [35S]GTPgammaS binding
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Inhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamineInhibition of human Histamine H3 receptor using [3H]N-alpha-methyl histamine
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Effect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptorEffect on specific [35S]GTP-gamma-S, Binding to HEK293 cell membranes expressing the human Histamine H3 receptor
Agonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation countingAgonist activity at human H3 receptor expressed in insect Sf9 cells co-expressing Gialpha2, Gbeta1gamma2 and RGS4 assessed as gamma[32P]GTP binding by liquid scintillation counting
Agonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assayAgonist activity at human histamine H3 receptor expressed in Sf9 cells coexpressing Gialpha-2-Gbeta-1-gamma-2 and RGS4 proteins protein by steady-state GTPase assay
Inhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptorInhibition of the forskolin-stimulated cAMP production in SK-N-MC cells expressing human Histamine H3 receptor
Agonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assayAgonist activity at human histamine H3 receptor expressed in sf9 cell membrane co-expressing mammalian Galphai2 and Gbeta1gamma2 incubated for 90 mins by [35S]GTPgammaS binding assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assayAntagonist activity at human H3 receptor expressed in HEK293 cells centrifuged for 3 mins followed by 60 mins incubation by LANCE Ultra cAMP assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor by GTPgammaS binding assayInverse agonist activity at human histamine H3 receptor by GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Inverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assayInverse agonist activity at human cloned histamine H3 receptor by [35S]GTPgammaS binding assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assayAntagonist activity at human H3 receptor expressed in CHOK1 cells incubated for 10 mins by HTRF assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.Histamine H3 receptor agonist activity was assessed by the inhibition of the electrically evoked twitch response of the guinea-pig ileum.
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Inverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assayInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding by cell-based assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Antagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomesAntagonist activity at histamine H3 receptor in rat forebrain assessed as inhibition of [3H]histamine release from synaptosomes
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).HTRF cAMP Assay: Compounds of the present invention were evaluated using the human H3 receptor (H3R) HTRF cAMP assay. In this assay, HEK293 cells expressing the human H3 receptor were suspended in PBS containing 100 μM IBMX and plated into 384-well assay plates (Perkin Elmer Proxiplate 384-Plus; 15,000 cells per well; 5 μL plating volume) and allowed to equilibrate for an hour. Test compounds were serially diluted in 100% DMSO and then further diluted in PBS containing forskolin (2 μM). Test compounds (5 μL) were then added to the assay plate and the mixture was incubated for 1 hour. HTRF assay reagents (Cisbio, Dynamic 2 cAMP Kit), cAMP-d2 and cryptate-labeled anti-cAMP antibody, are mixed with cell lysis buffer and added to the assay plate. After 1-hour incubation with these reagents, the assay plate was read on an HTRF-compatible microplate reader (Perkin Elmer EnVision or BMG Pherastar).
Modulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assayModulation of human histamine H3 receptor expressed in HEK293 cells assessed as change in forskolin-stimulated cAMP level after 1 hr by HTRF assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Inhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technologyInhibition of human H3R expressed in methylhistamine-induced human H3-bla U2OS cells incubated for 30 mins by beta-lactamase complementation technology
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.SPA Assay: The H3 binding assay was/can be used to evaluate the ability of at least one compound in accordance with formula I, Ia, Ib, and/or Ic to inhibit [3H]-N-α-methylhistamine binding to CHO-K1 membranes expressing human histamine H3 receptors (full-length H3, the most prevalent brain isoform 445). In 200 μl 96-well SPA format, human H3 membranes (12.5 μg protein/well) and 1.4 nM [3H]-N-α-methylhistamine were/can be incubated with at least one compound in accordance with formula I, Ia, Ib, and/or Ic for 1.5 hrs to determine percent effect with respect to total (1% DMSO) and non-specific binding (10 μM imetit). Reproducibility of the assay is such that IC50 curves can be generated in singlicate.
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells preincubated for 5 mins followed by forskolin-stimulation and measured after 5 hrs by CRE-driven luciferase reporter gene assay
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Inverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of N-alpha-methylhistamine-induced [35S]GTPgammaS binding
Guanosine 5'-O-(3-[35S]thio)triphosphate [GTP gamma S] Binding Assay: A GTP gamma S binding assay can be used to investigate antagonist properties of compounds in CHO cells (Chinese Hamster Ovary) transfected with human Histamine H3 receptor (hH3R). Membranes from CHO cells expressing hH3R (10 ug/well) are diluted in GTP gamma S assay buffer (20 mM Hepes, 10 mM MgCl2, 100 mM NaCl, pH 7.4) and preincubated with saponine (3 ug/ml), GDP (10 uM) and PVT-WGA SPA beads (125 ug/well) (Amersham) for 30 minutes. To determine antagonist activity, (R)-methyl histamine (30 nM) is added in 96 well SPA plate with [35S]GTP gamma S (0.2 nM) and various concentration of H3R antagonists. The GTP gamma S binding assay is started with addition of the mixture membrane/saponine/GDP and incubated for 90 minutes at room temperature. The amount of bound [35S]GTP gamma S is determined by using the MicroBeta Trilux counter (PerkinElmer). The percentage of [35S]GTP gamma S bound in each sample is calculated as a percentage of that bound control sample.Guanosine 5'-O-(3-[35S]thio)triphosphate [GTP gamma S] Binding Assay: A GTP gamma S binding assay can be used to investigate antagonist properties of compounds in CHO cells (Chinese Hamster Ovary) transfected with human Histamine H3 receptor (hH3R). Membranes from CHO cells expressing hH3R (10 ug/well) are diluted in GTP gamma S assay buffer (20 mM Hepes, 10 mM MgCl2, 100 mM NaCl, pH 7.4) and preincubated with saponine (3 ug/ml), GDP (10 uM) and PVT-WGA SPA beads (125 ug/well) (Amersham) for 30 minutes. To determine antagonist activity, (R)-methyl histamine (30 nM) is added in 96 well SPA plate with [35S]GTP gamma S (0.2 nM) and various concentration of H3R antagonists. The GTP gamma S binding assay is started with addition of the mixture membrane/saponine/GDP and incubated for 90 minutes at room temperature. The amount of bound [35S]GTP gamma S is determined by using the MicroBeta Trilux counter (PerkinElmer). The percentage of [35S]GTP gamma S bound in each sample is calculated as a percentage of that bound control sample.
Inverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS bindingInverse agonist activity at human cloned histamine H3 receptor assessed as inhibition of (R)-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Displacement of [3H]-N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting methodDisplacement of [3H]-N-alpha-methylhistamine from recombinant human histamine H3 receptor expressed in CHO-K1 cell membranes measured after 30 mins by microbeta scintillation counting method
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed as inhibition of calcium mobilization by FLIPR assay
Displacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cellsDisplacement of [125H]iodoproxyphan from human histamine H3 receptor expressed in CHO-K1 cells
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against human histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS bindingAntagonist activity at human cloned histamine H3 receptor expressed in CHO-K1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Antagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assayAntagonist activity at human histamine H3 receptor long form expressed in CHOK1 cells assessed as inhibition of R-alpha-methylhistamine-induced [35S]GTPgammaS binding after 3 hrs by scintillation proximity assay
Activity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cellsActivity against human H3 receptor as measured by CRE-mediated beta galactosidase reporter gene assay in forskolin-stimulated SK-N-MC cells
Antagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assayAntagonist activity at human histamine H3 receptor stably expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by Eu-cAMP tracer based TR-FRET assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assayAntagonist activity at human histamine H3 receptor expressed in HEK293 cells assessed by forskolin induced cAMP response element activation after 5 hrs by luciferase reporter gene assay
Antagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assayAntagonist activity against mouse histamine H3 receptor expressed in human HT1080 cells assessed as inhibition of (R)-alpha-methylhistamine-induced increase in intracellular calcium level by FLIPR assay
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
Antagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assayAntagonist activity at recombinant human Gi-coupled H3 receptor expressed in HEK293T cells assessed as reduction in histamine-induced inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 to 15 followed by histamine addition for 10 mins and subsequent forskolin-stimulation by Glo-sensor assay
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay
Antagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassayAntagonist activity at human histamine H3 receptor expressed in CHO cells assessed as inhibition of forskolin/R-alpha-methylhistamine-induced cAMP accumulation after 1.5 hrs by TR-FRET immunoassay