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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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. |
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V101613 | (S)-Setastine | (S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent H1 receptor antagonist. | |
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V86642 | (±)-Carbinoxamine | 486-16-8 | (±)-Carbinoxamine is a histamine H1 receptor antagonist. |
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V106767 | 1-Methyl-4-imidazoleacetic acid hydrochloride | 35454-39-8 | 1-Methyl-4-imidazoleacetic acid hydrochloride is a stable metabolite of histamine, produced by oxidation of the major metabolite N-methylhistamine. |
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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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V103785 | ADS031 | ADS031 is a histamine H3R antagonist with an affinity of 12.5 nM for hH3R and has the highest inhibitory activity against AChE (IC50 = 1.537 μM). | |
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V105060 | ADS1017 | ADS1017 is a histamine receptor and muscarinic receptor antagonist with good affinity for hH3R, hH4R, hM2R, and hM4R with pKi of 6.8, 5.5, 7.4, and 7.2, respectively. | |
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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. |
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V103940 | Arpromidine | 106669-71-0 | Apromidine (BU-E-50) is a histamine H2 receptor agonist and histamine H1 receptor antagonist. |
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V90046 | Bisfentidine | 96153-56-9 | Bisfentidine is an H2 receptor antagonist. |
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V104821 | BL 6341A | 78441-84-6 | BL 6341A is a histamine H2 receptor antagonist with Ki values of 3.5-4.4 nM, which inhibits histamine-induced acid secretion and cAMP formation. |
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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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V107254 | Cetirizine N-oxide | 1076199-80-8 | Cetirizine N-oxide is an oxidative degradation product of the histamine H1 receptor antagonist cetirizine. |
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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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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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