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 |
|---|---|---|---|---|
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V86642 | (±)-Carbinoxamine | 486-16-8 | (±)-Carbinoxamine is a histamine H1 receptor antagonist. |
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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. |
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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. | |
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V90046 | Bisfentidine | 96153-56-9 | Bisfentidine is an H2 receptor antagonist. |
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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. |
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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. |
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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. |
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V83847 | Enerisant hydrochloride (TS-091 hydrochloride) | 1152749-07-9 | |
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V79407 | Fexofenadine-d3 (MDL-16455-d3; Terfenadine carboxylate-d3) | Fexofenadine-d3 is the deuterated form of Fexofenadine. | |
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V2939 | GSK189254A | 720690-73-3 | GSK189254A (also known as GSK189254) is a novel histamine H(3) receptor antagonist with high affinity for human (pK(i) = 9.59 -9.90) and rat (pK(i) = 8.51-9.17) H(3) receptors. |
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V87063 | Histamine receptors inhibitor 1 | 744270-00-6 | Histamine receptors inhibitor 1 is a H1R or H4R inhibitor, which can be used in the research of inflammation, autoimmunity, allergy and eye. |
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V83547 | HY-078020 | 2756222-90-7 | |
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V86868 | JNJ 10181457 dihydrochloride | 544707-20-2 | JNJ-10181457 is a neutral, potent, brain-penetrant and selective non-imidazole H3 receptor antagonist that increases NE and acetylcholine concentrations in the rat frontal cortex. |
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V4515 | JNJ-31001074 | 929622-08-2 | Bavisant (also known as JNJ-31001074) is a novel, highly selective, orally bioactive antagonist of the human H3 receptor with a novel mechanism of action which involves wakefulness and cognition. |
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V4499 | JNJ-39758979 | 1046447-90-8 | JNJ-39758979 is a novel, potent and selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM. |
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V1239 | JNJ-7777120 | 459168-41-3 | JNJ-7777120 (JNJ7777120; JNJ 7777120), an indole analog, is a potent and selective non-imidazole-based histamine H4R receptor antagonist that can reduce allergic and asthmatic symptoms. |
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V37611 | LML134 | 1542135-76-1 | LML134 is a novel, orally bioactive and highly selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. |
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V29682 | N-Acetylhistamine | 673-49-4 | N-Acetylhistamine is a histamine metabolite. |
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V79880 | Pheniramine-d6 maleate (Prophenpyridamine-d6 (maleate); Tripoton-d6 (maleate)) | Pheniramine-d6 (maleate) is the deuterium labelled form of Pheniramine maleate. | |
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V85428 | Pirdonium bromide | 35620-67-8 |
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