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 |
|---|---|---|---|---|
|
V70353 | Cetirizine methyl ester (Levocetiride Impurity 8) | 83881-46-3 | Cetirizine methyl ester is an impurity of Cetirizine. |
|
V70365 | Cimetidine-d3 (SKF-92334-d3) | 1185237-29-9 | Cimetidine-d3 is the deuterated form of Cimetidine. |
|
V70377 | Cipralisant (enantiomer) (GT-2331 (enantiomer)) | 223420-11-9 | Cipralisant (GT-2331) enantiomer is the enantiomer of Cipralisant, an orally bioactive, specific, high-affinity histamine H3 receptor antagonist (rat Ki=0.47 nM). |
|
V8610 | Ciproxifan maleate (FUB-359) | 184025-19-2 | Ciproxifan (formerly known as FUB-359) is a highly potent and selective histamine H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes. |
|
V70331 | Cyclizine hydrochloride | 303-25-3 | Cyclizine HCl, a piperazine analogue, is a potent and specific histamine H1 receptor antagonist. |
|
V70321 | Dimaprit dihydrochloride | 23256-33-9 | Dimaprit di-HCl is a selective histamine H2 receptor agonist that also inhibits nNOS with IC50 of 49 μM. |
|
V70335 | Dioxopromethazine (Prothanon; 9,9-Dioxopromethazine; 9,9-Dioxypromethazin) | 13754-56-8 | Dioxopromethazine is an orally bioactive antihistamine. |
|
V70311 | Dothiepin (Dosulepin; Dothep) | 113-53-1 | Dothiepin (Dosulepin; Dothep) is an antidepressant with sedative/anxiolytic activity. |
|
V70366 | Doxylamine | 469-21-6 | Doxylamine, a first-generation antihistamine, is a histamine (H1) receptor blocker (antagonist). |
|
V70330 | Ebastine-d5 (Ebastine d5) | 1216953-13-7 | Ebastine-d5 is the deuterium labelled form of Ebastine. |
|
V70344 | Granuliberin R | 64704-41-2 | Granuliberin R is a new mast cell degranulation peptide extracted from amphibians and can be extracted from the skin of frog (Rana rugosa). |
|
V70319 | H3R antagonist 1 hydrochloride | 2319790-07-1 | H3R antagonist 1 HCl is a potent histamine receptor 3 (H3R) inverse agonist. |
|
V70337 | H4R antagonist 2 | 1148115-99-4 | H4R antagonist 2 (page 68) is a Furo[3,2-d]pyrimidine analogue and is a potent H4R antagonist. |
|
V70378 | H4R antagonist 3 | 1003091-20-0 | H4R antagonist 3 (Example 18) is a histamine-4 receptor antagonist (inhibitor) with EC50 <10 mM. |
|
V70352 | Histamine H4 receptor antagonist-1 | 1246207-84-0 | Histamine H4 receptor antagonist-1 is an H4 histamine receptor antagonist. |
|
V70333 | HTMT dimaleate | 195867-54-0 | HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. |
|
V70336 | Hydroxyzine-d4 dihydrochloride (Vistaril-d4' (dihydrochloride); Atarax-dd4' (dihydrochloride)) | 1219805-91-0 | Hydroxyzine-d4 (di-HCl) is the deuterium labelled form of Hydroxyzine di-HCl. |
|
V70340 | Hydroxyzine-d8 dihydrochloride (hydroxyzine d8 hydrochloride (bis hydrochloride)) | 1808202-93-8 | Hydroxyzine-d8 (di-HCl) is the deuterium labelled form of Hydroxyzine di-HCl. |
|
V70375 | ICI 162846 | 84545-30-2 | ICI 162846 is an orally bioactive antagonist of H2 receptors. |
|
V70338 | Immepi | 151070-83-6 | Immepip is an H3 agonist. |
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