1. GPCR/G Protein
  2. Histamine Receptor

Histamine Receptor

Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.

Histamine Receptor Related Products (82):

Cat. No. Product Name Effect Purity
  • HY-13980
    UNC0642 Inhibitor
    UNC0642 is a potent and selective G9a/GLP inhibitor, inhibits G9a/GLP with an IC50 of less than 2.5 nM.
  • HY-12199B
    Pitolisant hydrochloride Antagonist
    Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
  • HY-N0054
    Osthole Inhibitor
    Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.
  • HY-30234A
    Clemizole hydrochloride Antagonist
    Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. The IC50 of Clemizole for RNA binding by NS4B is 24±1 nM, whereas its EC50 for viral replication is 8 µM.
  • HY-A0015
    Bepotastine Beslilate Antagonist
    Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.
  • HY-14111
    GSK189254A Antagonist
    GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
  • HY-17039
    Alcaftadine Antagonist
    Alcaftadine(R89674) is a H1 histamine receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis.
  • HY-13508
    JNJ-7777120 Antagonist
    JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.
  • HY-14447
    Bilastine Antagonist
    Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria.
  • HY-17042A
    Cetirizine dihydrochloride Inhibitor
    Cetirizine 2Hcl, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.
  • HY-15538
    Ebrotidine Antagonist
    Ebrotidine(FI 3542) is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection.
  • HY-17043
    Loratadine Agonist
    Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
  • HY-15540
    Metiamide Antagonist
    Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide.
  • HY-14289
    Cimetidine Antagonist
    Cimetidine is a histamine-2 (H2) receptor antagonist.
  • HY-15541
    Zaltidine Antagonist
    Zaltidine(CP-57361) is a H2-receptor antagonist, which has the antisecretory action.
  • HY-15289
    Ciproxifan maleate Antagonist
    Ciproxifan maleate(FUB-359 maleate) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.
  • HY-17428
    Tripelennamine hydrochloride Antagonist
    Tripelennamine Hcl, a H1-receptor antagonist, is a psychoactive drug and member of the pyridine andethylenediamine classes that is used as an antipruritic and first-generation antihistamine.
  • HY-14880B
    Bavisant dihydrochloride hydrate Antagonist
    Bavisant Hcl hydrate(JNJ-31001074) is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
  • HY-12195
    ABT-239 Antagonist
    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. 
  • HY-12199
    Pitolisant Inhibitor
    Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).