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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V103285 | Donetidine | 99248-32-5 | Donetidine (SK&F 93574) is a histamine H2 receptor antagonist that enhances histamine release in the beagle dog model. |
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V107689 | Elbanizine | 110629-41-9 | Albanizine inhibits histamine, bradykinin activity, histamine release from rat mast cells (IC50 0.26 μM), and IgE-mediated passive cutaneous anaphylaxis (PCA). |
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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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V98714 | H3R antagonist 1 | 1448422-61-4 | H3R-IN-1 is a potent histamine receptor 3 (H3R) inverse agonist. |
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V105883 | Histamine dehydrogenase, Microorganism | 89190-47-6 | Histamine dehydrogenase, microbial (EC 1.4.99) is a homodimeric enzyme that catalyzes the oxidative deamination of histamine in the presence of an electron carrier. |
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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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V94342 | Impromidine hydrochloride | 65573-02-6 | Imoprodine is a potent histamine H2 receptor agonist. |
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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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V107392 | Meclizine N-oxide | 114624-69-0 | Meclizine N-oxide is a metabolite of the histamine H1 receptor antagonist meclizine. |
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V102521 | Methimepip dihydrobromide | 817636-54-7 | Methimepip dihydrobromide is a potent and selective histamine H3 receptor agonist with EC50 of 0.316 nM. |
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V29682 | N-Acetylhistamine | 673-49-4 | N-Acetylhistamine is a histamine metabolite. |
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V94254 | Noberastine maleate | 111922-05-5 | Norbestin maleate is a potent histamine H1 antagonist. |
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V102493 | Oxmetidine | 72830-39-8 | Ometidine (SKF 92994) is an orally active H2 receptor antagonist and antiulcer agent. |
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