Signaling Pathway

Histamine Receptor

Histamine Receptor

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Histamine receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.

Histamine Receptor Inhibitors & Modulators (81)

Product Name Catalog No. Brief Description
(±)-Methotrimeprazine D6

HY-19489S

(±)-Methotrimeprazine (D6) is the deuterium labeled Methotrimeprazine, which is a D3 dopamine and Histamine H1 receptor antagonist.

ABT-239

HY-12195

ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist.

Alcaftadine

HY-17039

Alcaftadine(R89674) is a H1 histamine receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis.

Antazoline hydrochloride

HY-B1067

Antazoline hydrochloride is a 1st generation antihistamine with also anticholinergic properties used to relieve nasal congestion and in eye drops.

Azatadine

HY-B0170

Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.

Azatadine dimaleate

HY-B0170A

Azatadine dimaleate is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.

Azelastine

HY-B0462A

Azelastine is a potent, second-generation, selective, histamine antagonist.

Azelastine hydrochloride

HY-B0462

Azelastine HCl is a potent, second-generation, selective, histamine antagonist.

Bavisant

HY-14880

Bavisant (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.

Bavisant dihydrochloride

HY-14880A

Bavisant Hcl (JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.

Bavisant dihydrochloride hydrate

HY-14880B

Bavisant Hcl hydrate(JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.

Bepotastine Beslilate

HY-A0015

Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.

Betahistine dihydrochloride

HY-B0524A

Betahistine Dihydrochloride is a histamine H3 receptors inhibitor used as an antivertigo drug.

Bilastine

HY-14447

Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria.

Brompheniramine maleate

HY-B0480

Brompheniramine maleate is a histamine H1 receptors antagonist.

Cetirizine

HY-17042

Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.

Cetirizine D4 dihydrochloride

HY-17042AS

Cetirizine D4 2Hcl is deuterium labeled Cetirizine, which is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist.

Cetirizine D8 dihydrochloride

HY-17042AS1

Cetirizine D8 2Hcl is deuterium labeled Cetirizine, which is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist.

Cetirizine dihydrochloride

HY-17042A

Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.

Chlorpheniramine maleate

HY-B0286A

Chlorpheniramine maleate is an histamine H1 receptor antagonist with IC50 of 12 nM.