Histamine serves as the endogenous ligand for the class of G protein-coupled receptors known as histamine receptors. The H1 receptor, H2 receptor, H3 receptor, and H4 receptor are the four recognized histamine receptors. A member of the family of G-protein-coupled receptors that resemble Rhodopsin is the histamine receptor H1. This receptor, specifically expressed in smooth muscles, vascular endothelial cells, the heart, and the central nervous system, is triggered by the biogenic amine histamine and is found throughout the body. Gs mediates the positive coupling of H2 receptors to adenylate cyclase. It is a strong inducer of cAMP synthesis, which activates Protein Kinase A. Histamine H3 receptors act as autoreceptors in presynaptic histaminergic neurons and regulate histamine turnover by feedback inhibition of histamine synthesis and release. They are expressed in the central nervous system and to a lesser extent the peripheral nervous system. It has been demonstrated that the mast cell chemotaxis and eosinophil shape change are both mediated by the histamine H4 receptor.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V70329 | (R)-Meclizine | 189298-48-4 | (R)-Meclizine is the R form enantiomer of Meclizine. |
|
V70364 | (Z)-Lafutidine ((Z)-FRG-8813) | 206449-93-6 | (Z)-Lafutidine ((Z)-FRG-8813) is a histamine H2 receptor antagonist that exerts mucoprotective effects on sensory afferent neurons and has antisecretory and gastroprotective activities. |
|
V70328 | 4'-O-Methylnyasol (Ellisinin A) | 79004-25-4 | 4'-O-Methylnyasol is an inhibitor (blocker/antagonist) of β-hexosaminidase. |
|
V70347 | 4-Methylhistamine | 36507-31-0 | 4-Methylhistamine is a potent agonist of the histamine 4 receptor (H4R). |
|
V70315 | 4-Methylhistamine dihydrochloride | 36376-47-3 | 4-Methylhistamine (di-HCl) is a potent agonist of the histamine 4 receptor (H4R). |
|
V70326 | 4-Methylhistamine hydrochloride | 84103-51-5 | 4-Methylhistamine ( HCl) is a potent, high-affinity H4 receptor agonist. |
|
V70327 | A-943931 | 1027330-97-7 | A-943931 is a potent and specific histamine H4 receptor antagonist (inhibitor) with Kis of 4.6 and 3.8 nM for human and rat H4R, respectively. |
|
V70332 | A-987306 | 1082954-71-9 | A-987306 is a highly effective, orally bioactive histamine H4 antagonist (inhibitor) with Kis of 3.4 nM and 5.8 nM for rat and human H4, respectively. |
|
V10690 | Alcaftadine (R-89674) | 147084-10-4 | Alcaftadine (R89674; R-89674;trade name Lastacaft) is a potent H1 histamine receptor antagonistused as a topical medication to prevent eye irritation caused by allergic conjunctivitis. |
|
V8045 | Betahistine | 5638-76-6 | Betahistine (also known as PT-9) is a potent histamine H3 receptor inhibitor with IC50 of 1.9 μM. |
|
V70346 | Betahistine-d3 dihydrochloride (Betahistine-d3 dihydrochloride) | 244094-72-2 | Betahistine-d3 (di-HCl) is the deuterium labelled form of Betahistine di-HCl. |
|
V70312 | Betazole (Ametazole) | 105-20-4 | Betazole (Ametazole) is a pyrazole histamine and an orally bioactive H2 receptor agonist. |
|
V70345 | Betazole dihydrochloride (Ametazole dihydrochloride) | 138-92-1 | Betazole (Ametazole) di-HCl is a pyrazole histamine and an orally bioactive H2 receptor agonist. |
|
V70339 | Bilastine-d6 (Bilastine d6) | 1215358-58-9 | Bilastine-d6 is the deuterated form of Bilastine. |
|
V70349 | Bufrolin | 54867-56-0 | Bufrolin is a Cromoglycate (histamine release inhibitor) analogue and a potent GPR35 agonist. |
|
V70369 | Carcinine (β-Alanylhistamine) | 56897-53-1 | Alistin (Carcinine; β-Alanylhistamine) is a selective histamine H3 (histamine H3) antagonist (inhibitor) with anti-oxidant effect and neuro-protection effects on oxidative stress mouse retina. |
|
V70350 | Carebastine-d5 (Carebastine d5) | 1189661-02-6 | Carebastine-d5 is the deuterium labelled form of Carebastine. |
|
V70351 | Carebastine-d5 Methyl Ester | 1190019-51-2 | Carebastine-d5 Methyl Ester is the deuterium labelled form of Carebastine. |
|
V70317 | Cetirizine Impurity C | 83881-59-8 | Cetirizine Impurity C is an impurity in Cetirizine. |
|
V70357 | Cetirizine Impurity D | 346451-15-8 | Cetirizine Impurity D is the impurity of Cetirizine. |
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