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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V4572 | SUN-1334H | 607736-84-5 | SUN 1334H is a novel, potent, orally bioactive, and highly selectiveH1 receptorantagonist withKiof 9.7 nM. |
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V1232 | Tetrandrine (NSC-77037) | 518-34-3 | Tetrandrine (also called Fanchinine; Sinomenine A; d-tetrandrine; formerly NSC-77037), a bis-benzylisoquinoline alkaloid derived from Stephania tetrandra, is a novel and potent calcium channel blocker which inhibits voltage-gated Ca2+ current (ICa) and Ca2+-activated K+ current. |
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V1237 | Tripelennamine HCl | 154-69-8 | Tripelennamine HCl (Pyrinamine; Stanzamine; Tripelennamine; Pyribenzamine), the hydrochloride salt of Tripelennamine, is a potent histamine H1 receptor antagonist that has been widely used as an antipruritic agent. |
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V3236 | VUF10460 | 1028327-66-3 | VUF10460 is a non-imidazole agonist of the histamine H4 receptor which binds to rat H4 receptor with a pKi of 7.46. |
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