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 |
|---|---|---|---|---|
|
V70342 | Immethridine dihydrobromide | 699020-93-4 | Immethridine diHBr is a selective histamine H3 receptor (H3R) agonist. |
|
V4311 | JNJ-5207852 | 398473-34-2 | JNJ-5207852 is a novel and potent histamine antagonist selective for the H3 subtype. |
|
V70334 | JNJ-5207852 dihydrochloride | 1782228-76-5 | JNJ-5207852 di-HCl is a selective and effective antagonist of histamine H3 receptors. |
|
V70355 | Mianserin-d3 hydrochloride (Org GB 94-d3) | 1219804-97-3 | Mianserin-d3 ( HCl) is the deuterated form of Mianserin HCl. |
|
V70318 | MK-0249 | 862309-06-6 | MK-0249 (Compound 1) is a specific, orally bioactive histamine H3 receptor antagonist (inhibitor) with IC50 of 1.7 nM for human H3 receptors. |
|
V70324 | N-Desmethyl diphenhydramine-d3 hydrochloride | 1794759-12-8 | N-Desmethyl diphenhydramine-d3 (HCl) is deuterated labeled N-Desmethyl diphenhydramine HCl. |
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V70314 | Niaprazine | 27367-90-4 | Niaprazine is a histamine H1-receptor antagonist. |
|
V70368 | Nizatidine-d3 (Nizatidine d3) | 1246833-99-7 | Nizatidine-d3 is the deuterated form of Nizatidine. |
|
V70376 | Olopatadine-d3 hydrochloride (Olopatadine d3 hydrochloride (hydrochloride)) | 1331635-21-2 | Olopatadine-d3 ( HCl) is the deuterated form of Olopatadine HCl. |
|
V70381 | Onitin (金粉 fern pavilion) | 53823-02-2 | Onitin is a naturally occurring compound that can be extracted from Onychium siliculosum. |
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V70322 | Oxomemazine | 3689-50-7 | Oxomemazine is a phenothiazine-based histamine H1-receptor antagonist (blocker) with significant antimuscarinic activity. |
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V70374 | Panaxydiol | 63910-76-9 | Panaxydiol has the activity of inhibiting the release of histamine. |
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V4310 | PF-03654746 | 935840-31-6 | PF-03654746 is a novel, potent,specific and selective histamine H3 receptor antagonist with >1000-fold selectivity for the H 3 receptor over the other histamine receptor subtypes. |
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V70320 | PF-03654764 | 935840-35-0 | PF-03654764 is an orally bioactive, selective histamine H3 receptor antagonist (inhibitor) with Kis of 1.2 nM and 7.9 nM for human H3 and rat H3, respectively. |
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V70372 | Phenindamine (Nu 1504) | 82-88-2 | Phenindamine (Nu 1504) is an antihistamine. |
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V4308 | PITOLISANT HCL | 903576-44-3 | Pitolisant HCl (formerly also known as BF2.649; BF2649; Ciproxidine; Wakix) is a nonimidazole-based inverse agonist of the recombinant humanhistamine H3 receptorapproved in 2019 for the treatment of excessive daytime sleepiness in adults with narcolepsy. |
|
V4309 | PITOLISANT OXALATE | 362665-57-4 | Pitolisant oxalate (formerly BF2649;BF2.649; Ciproxidine;Tiprolisant; Wakix), the oxalate salt of pitolisant, is a novel nonimidazole analog and an inverse agonist of the recombinant humanhistamine H3 receptorwith Kiof 0.16 nM. |
|
V70363 | Promethazine-d4 hydrochloride (Promethazine d4 hydrochloride) | 1173018-74-0 | Promethazine-d4 ( HCl) is the deuterated form of Promethazine HCl. |
|
V70325 | Promethazine-d6 hydrochloride ((±)-Promethazine-d6 (hydrochloride)) | 1189947-02-1 | Promethazine-d6 ( HCl) is the deuterated form of Promethazine HCl. |
|
V70362 | Propiomazine | 362-29-8 | Propiomazine is an orally bioactive antihistamine with sedative properties. |
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