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Histamine Receptor

Histamine Receptor

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.

Histamine Receptor related products

Structure Cat No. Product Name CAS No. Product Description
(R)-(+)-Mequitazine V98157 (R)-(+)-Mequitazine 147780-50-5 (R)-(+)-Mequitazine is a histamine H1 receptor antagonist that is biotransformed primarily through human liver microsomes to produce hydroxylated and S-oxidized metabolites.
(S)-Setastine V101613 (S)-Setastine (S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent H1 receptor antagonist.
(±)-Carbinoxamine V86642 (±)-Carbinoxamine 486-16-8 (±)-Carbinoxamine is a histamine H1 receptor antagonist.
1-Methyl-4-imidazoleacetic acid hydrochloride V106767 1-Methyl-4-imidazoleacetic acid hydrochloride 35454-39-8
ABT-239 V4406 ABT-239 460746-46-7 ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist/inverse agonist developed by Abbott with stimulant and nootropic effects, and has been investigated as a treatment for ADHD, Alzheimer's disease, and schizophrenia.
ADS031 V103785 ADS031
ADS1017 V105060 ADS1017
Aminopotentidine V97373 Aminopotentidine 140873-26-3 Aminopotentidine is a histamine H2 receptor antagonist with KB values of 220 and 280 nM for human and guinea pig H2 receptors, respectively.
Anticancer agent 192 V89035 Anticancer agent 192 Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist that has no affinity for muscarinic and hERG.
APD-916 V101866 APD-916 1021169-11-8 APD-916 is an H3 receptor antagonist.
Arpromidine V103940 Arpromidine 106669-71-0
Bisfentidine V90046 Bisfentidine 96153-56-9 Bisfentidine is an H2 receptor antagonist.
BL 6341A V104821 BL 6341A 78441-84-6
BMY-25368 hydrochloride V86638 BMY-25368 hydrochloride 86134-36-3 BMY-25368 hydrochloride is a histamine H2 receptor antagonist and can be used as a gastric acid secretion inhibitor.
Carcinine dihydrochloride V101252 Carcinine dihydrochloride 57022-38-5 Carcinine (β-alanylhistamine) dihydrochloride is a selective histamine H3 antagonist with antioxidant activity and neuroprotective effects on the retina of oxidatively stressed mice.
Cetirizine N-oxide V107254 Cetirizine N-oxide 1076199-80-8
Ciproxifan hydrochloride V92291 Ciproxifan hydrochloride 1049741-81-2 Ciproxifan (FUB 359) hydrochloride is a potent, selective, orally active and competitive histamine H3-receptor antagonist with IC50 of 9.2 nM.
CP19 V56025 CP19 1018148-68-9 CP19 is a histamine receptor antagonist and an entry inhibitor for Ebola virus (EBOV) and Marburg virus (MARV), with IC50s of 3.4 μM and 29.5 μM respectively.
Dioxopromethazine hydrochloride V102215 Dioxopromethazine hydrochloride 15374-15-9 Dioxin is an oral antihistamine.
Dioxopromethazine hydrochloride (Standard) V97054 Dioxopromethazine hydrochloride (Standard) 15374-15-9 Dioxin Hydrochloride (Standard) is the analytical standard for Dioxin Hydrochloride.
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