1. GPCR/G Protein
    Immunology/Inflammation
  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 (113):

Cat. No. Product Name Effect Purity
  • HY-17043
    Loratadine Agonist 99.95%
    Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
  • HY-12199B
    Pitolisant hydrochloride Antagonist 99.22%
    Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
  • HY-14289
    Cimetidine Antagonist >98.0%
    Cimetidine is a histamine-2 (H2) receptor antagonist.
  • HY-N0054
    Osthole Inhibitor 99.81%
    Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.
  • HY-B0298A
    Clemastine fumarate Antagonist 99.82%
    Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
  • HY-101189
    JNJ-39758979 Antagonist 98.01%
    JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM.
  • HY-100280
    Pirolate Antagonist
    Pirolate is a histamine H1 receptor.
  • HY-100238
    Antihistamine-1 Inhibitor
    Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
  • HY-13508
    JNJ-7777120 Antagonist >98.0%
    JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.
  • HY-30234A
    Clemizole hydrochloride Antagonist 99.70%
    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-A0077
    Perphenazine Inhibitor 99.93%
    Perphenazine is a typical antipsychotic drug, inhibits 5-HT2A receptor (5-HT2A), Alpha-1A adrenergic receptor (α1A), Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor (H1) with Ki of 5.6, 10, 0.765/0.13, 3.4, and 8 nM.
  • HY-B1204
    Histamine Activator
    Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
  • 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-B0539
    Desloratadine Antagonist 99.75%
    Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.
  • HY-B0377
    Famotidine Antagonist 98.17%
    Famotidine is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
  • HY-15289
    Ciproxifan maleate Antagonist 99.56%
    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-17042A
    Cetirizine dihydrochloride Inhibitor 99.17%
    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-B0462
    Azelastine hydrochloride Antagonist 99.95%
    Azelastine HCl is a potent, second-generation, selective, histamine antagonist.
  • HY-14537
    Latrepirdine dihydrochloride Antagonist 99.75%
    Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β () secretion.
  • HY-12195
    ABT-239 Antagonist 98.94%
    ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. 
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