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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.
(R)-Meclizine V70329 (R)-Meclizine 189298-48-4 (R)-Meclizine is the R form enantiomer of Meclizine.
(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.
(Z)-Lafutidine ((Z)-FRG-8813) V70364 (Z)-Lafutidine ((Z)-FRG-8813) 206449-93-6 (Z)-Lafutidine ((Z)-FRG-8813) is a histamine H2 receptor antagonist that exerts mucoprotective effects on sensory afferent neurons and has antisecretory and gastroprotective activities.
(±)-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.
4'-O-Methylnyasol (Ellisinin A) V70328 4'-O-Methylnyasol (Ellisinin A) 79004-25-4 4'-O-Methylnyasol is an inhibitor (blocker/antagonist) of β-hexosaminidase.
4-Methylhistamine V70347 4-Methylhistamine 36507-31-0 4-Methylhistamine is a potent agonist of the histamine 4 receptor (H4R).
4-Methylhistamine dihydrochloride V70315 4-Methylhistamine dihydrochloride 36376-47-3 4-Methylhistamine (di-HCl) is a potent agonist of the histamine 4 receptor (H4R).
4-Methylhistamine hydrochloride V70326 4-Methylhistamine hydrochloride 84103-51-5 4-Methylhistamine ( HCl) is a potent, high-affinity H4 receptor agonist.
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.
A-943931 V70327 A-943931 1027330-97-7 A-943931 is a potent and specific histamine H4 receptor antagonist (inhibitor) with Kis of 4.6 and 3.8 nM for human and rat H4R, respectively.
A-987306 V70332 A-987306 1082954-71-9 A-987306 is a highly effective, orally bioactive histamine H4 antagonist (inhibitor) with Kis of 3.4 nM and 5.8 nM for rat and human H4, respectively.
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).
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