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 |
|---|---|---|---|---|
|
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. |
|
V101613 | (S)-Setastine | (S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent H1 receptor antagonist. | |
|
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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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. |
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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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V101866 | APD-916 | 1021169-11-8 | APD-916 is an H3 receptor antagonist. |
|
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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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. |
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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. |
|
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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V102215 | Dioxopromethazine hydrochloride | 15374-15-9 | Dioxin is an oral antihistamine. |
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V97054 | Dioxopromethazine hydrochloride (Standard) | 15374-15-9 | Dioxin Hydrochloride (Standard) is the analytical standard for Dioxin Hydrochloride. |
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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. | |
|
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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V98714 | H3R antagonist 1 | 1448422-61-4 | H3R-IN-1 is a potent histamine receptor 3 (H3R) inverse agonist. |
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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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