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 (105):

Cat. No. Product Name Effect Purity
  • 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-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-N0054
    Osthole Inhibitor 99.81%
    Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity.
  • HY-14289
    Cimetidine Antagonist >98.0%
    Cimetidine is a histamine-2 (H2) receptor antagonist.
  • 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
    JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM. JNJ-39758979 has been studied in phase II clinical trials in asthma and atopic dermatitis.
  • HY-B1589A
    Carbinoxamine maleate salt Antagonist 99.78%
    Carbinoxamine maleate salt is a histamine H1 receptor antagonist.
  • HY-B1305
    Chloropyramine hydrochloride Antagonist 99.30%
    Chloropyramine hydrochloride is a histamine receptor H1 antagonist which can also inhibit the biochemical function of VEGFR-3 and FAK.
  • 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-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-B1204
    Histamine Activator 98.08%
    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-17043
    Loratadine Agonist 99.81%
    Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
  • HY-B0539
    Desloratadine Antagonist 99.91%
    Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.
  • HY-B0462
    Azelastine hydrochloride Antagonist 99.95%
    Azelastine HCl is a potent, second-generation, selective, histamine antagonist.
  • HY-B0970
    Diphenylpyraline hydrochloride Inhibitor 98.41%
    Diphenylpyraline Hcl is a first-generation antihistamine with anticholinergic effects, acts as a dopamine reuptake inhibitor, shows to be useful in the treatment of Parkinsonism.
  • 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-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-B0781
    Promethazine hydrochloride Antagonist 99.82%
    Promethazine Hcl(NSC-231688) is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.
  • 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-A0015
    Bepotastine Beslilate Antagonist 99.36%
    Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.