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Histamine Receptor

Histamine Receptor

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.

Histamine Receptor related products

Structure Cat No. Product Name CAS No. Product Description
(+)-Dropropizine V121176 (+)-Dropropizine 99291-24-4 (+)-Dropropizine is an isomer of fluproizine and is an orally effective histamine receptor inhibitor with anti-allergic effects.
(R)-(+)-Mequitazine 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.
(R)-Azelastine hydrochloride V121898 (R)-Azelastine hydrochloride 153408-28-7 (R)-Azelastine hydrochloride is an antihistamine that has been shown to downregulate the levels of H1R, M1R, and M3R while inhibiting the proliferation of HNEpC.
(S)-Cetirizine dihydrochloride V122155 (S)-Cetirizine dihydrochloride 163837-48-7 (S)-Cetirizine dihydrochloride is an orally effective histamine H1 receptor antagonist with a Ki value of 39.1 nM.
(S)-Setastine V101613 (S)-Setastine (S)-Setastine ((S)-EGIS-2062 free acid) is a non-sedating, highly potent H1 receptor antagonist.
(±)-Carbinoxamine V86642 (±)-Carbinoxamine 486-16-8 (±)-Carbinoxamine is a histamine H1 receptor antagonist.
1-Methyl-4-imidazoleacetic acid hydrochloride 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.
6-O-Senesioyl plenolin V127464 6-O-Senesioyl plenolin 90042-11-8 6-O-Senesioyl plenolin is a sesquiterpene lactone found in the small centipede (Centipeda minima) and has anti-allergic activity.
A-423579 V116249 A-423579 461045-17-0 A-423579 is an orally effective non-imidazolium histamine H3 receptor antagonist.
AA 344 V110927 AA 344 50743-49-2 AA 344 is an orally effective antihistamine.
ABT-239 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.
ADS031 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).
ADS1017 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.
Alinastine V114418 Alinastine 154541-72-7 Alistatin is a novel antihistamine.
Aminopotentidine 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.
Anticancer agent 192 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.
APD-916 V101866 APD-916 1021169-11-8 APD-916 is an H3 receptor antagonist.
Arpromidine V103940 Arpromidine 106669-71-0 Apromidine (BU-E-50) is a histamine H2 receptor agonist and histamine H1 receptor antagonist.
Asenapine-13C,d3 maleate V129494 Asenapine-13C,d3 maleate Asenapine-13C,d3 maleate is a deuterated 13C-asenapine maleate.
Bamipine V112327 Bamipine 4945-47-5 Bamipine is a potent histamine H1 receptor antagonist with moderate activity against Mycobacterium tuberculosis and also has a mild sedative effect.
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