H₃ Receptor Antagonist

H₃ Receptor Antagonists (26):

Cat. No.	Product Name	Effect	Purity

HY-12199B

Pitolisant hydrochloride	Antagonist	99.67%
Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

HY-14111

GSK189254A	Antagonist	98.09%
GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pK_i values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.

HY-107562

JNJ 10181457 dihydrochloride	Antagonist
JNJ-10181457 is a neutral, potent, brain-penetrant and selective non-imidazole H₃ antagonist which increases NE and ACh concentrations in rat frontal cortex. JNJ-10181457 can be used for neurological research.

HY-107557

Proxyfan	Antagonist
Proxyfan is a potent histamine H3 receptor antagonist with K_i values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan is over 1000-fold more potent at H3 receptors than other histamine receptors.

HY-107557A

Proxyfan Oxalate	Antagonist
Proxyfan Oxalate is a potent histamine H3 receptor antagonist with K_i values of 2.9 nM and 2.7 nM for rat and human H3 receptor, respectively. Proxyfan Oxalate is over 1000-fold more potent at H3 receptors than other histamine receptors.

HY-101232

Tiotidine	Antagonist	99.28%
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA₂=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.

HY-12195

ABT-239	Antagonist	99.23%
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.

HY-107566

Conessine	Antagonist	≥98.0%
Conessine, a steroidal alkaloid, is a potent and selective histamine H₃ receptor antagonist with K_is of 5.4, 6.0, 5.7 and 25 nM for human, dog, guinea pig, and rat H H₃ receptor, respectively. Anti-malarial activity.

HY-123532

JNJ10191584	Antagonist	99.95%
JNJ10191584 (VUF6002) is an orally active and selective histamine H₄ receptor antagonist with a K_i value of 26 nM. JNJ10191584 shows 540-fold selectivity to H₄ receptor over H₃ receptor with a K_i value of 14.1 μM. JNJ10191584 inhibits chemotaxis of eosinophils and mast cells with IC₅₀ values of 530 nM and 138 nM, respectively.

HY-109968

Irdabisant	Antagonist	99.38%
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment.

HY-12190

JNJ-5207852	Antagonist	≥98.0%
JNJ-5207852 is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

HY-12206A

Thioperamide maleate	Antagonist	98.26%
Thioperamide maleate (MR-12842 maleate) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a K_i of 4.3 nM for inhibition of [³H]histamine release. Thioperamide maleate inhibits [³H]histamine synthesis with a K_i of 31 nM.

HY-14880B

Bavisant dihydrochloride hydrate	Antagonist	99.26%
Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research.

HY-U00076

MK-0249	Antagonist	99.53%
MK-0249 (Compound 1) is a potent, selective and orally active histamine H₃ receptor antagonist, with an IC₅₀ of 1.7 nM for human H3.

HY-14880

Bavisant	Antagonist
Bavisant (JNJ-31001074) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H₃ receptor. Bavisant can be used for attention-deficit hyperactivity disorder (ADHD) research.

HY-107558

JNJ10191584 maleate	Antagonist
JNJ10191584 (VUF6002) maleate (compound 40) is an orally active and selective histamine H₄ receptor antagonist with a K_i value of 26 nM. JNJ10191584 maleate shows 540-fold selectivity to H₄ receptor over the H₃ receptor with a K_i value of 14.1 μM. JNJ10191584 maleate inhibits chemotaxis of eosinophils and mast cells with IC₅₀ values of 530 nM and 138 nM, respectively.

HY-19881

ABT-288	Antagonist
ABT-288 is a competitive, potent and selective histamine H3 receptor (H3R) antagonist. ABT-288 has K_i values of 1.9 and 8.2 nM for human and rat H3Rs, respectively. ABT-288 can be used in cognitive impairment research..

HY-12190A

JNJ-5207852 dihydrochloride	Antagonist
JNJ-5207852 dihydrochloride is a selective and potent histamine H₃ receptor (H₃R) antagonist, with pK_is of 8.9, 9.24 for rat and human H₃R, respectively.

HY-109968A

Irdabisant hydrochloride	Antagonist
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with K_i values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC₅₀ of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment.

HY-106000

GSK239512	Antagonist
GSK239512 is a potent and brain penetrated H₃ receptor antagonist. GSK239512 can be used for the research of mild-to-moderate Alzheimer's disease (AD).

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