H₃ Receptor

H₃ Receptor Related Products (37):

By Type:	Pan (11) Selective (18)
By Effects:	Inhibitors (2) Agonists (3) Antagonists (26) Modulators (6)

Cat. No.	Product Name	Effect	Purity

HY-B0527A

Amitriptyline hydrochloride	Inhibitor	98.91%
Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a K_i of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.

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-101198

Clobenpropit dihydrobromide	Modulator	98.99%
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC₅₀ of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (K_i 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (K_i 7.4 nM) and α2A/α2C adrenoceptors (K_i 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.

HY-B0524

Betahistine	Modulator	98.04%
Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA).

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-W014941

(R)-(-)-α-Methylhistamine dihydrochloride	Agonist	99.62%
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a K_d of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.

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-B0524A

Betahistine dihydrochloride	Modulator	99.82%
Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).

HY-D0237

Betahistine mesylate	Modulator	99.90%
Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine mesylate is used for the study of rheumatoid arthritis (RA).

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-112219A

H3R antagonist 1 hydrochloride	Inhibitor
H3R antagonist 1 hydrochloride is a histamine receptor 3 (H3R) inverse agonist extracted from patent WO2013107336A1, compound example 2.

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-101173

Imetit dihydrobromide	Agonist	≥98.0%
Imetit dihydrobromide (VUF 8325 dihydrobromide) is a high affinity and potent agonist of histamine H3 and H4 receptors, with K_i values of 0.3 and 2.7 nM, respectively. Imetit mimics histamine effect in triggering a shape change in eosinophils (EC₅₀=25 nM).

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-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.

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