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 (86):

Cat. No. Product Name Effect Purity
  • HY-13980
    UNC0642 Inhibitor 99.89%
    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 99.80%
    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.
  • HY-B0298A
    Clemastine fumarate Antagonist 99.80%
    Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
  • HY-B1510
    Acrivastine Inhibitor 98.00%
    Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.
  • HY-101420
    VUF10460 Agonist 98.37%
    VUF10460 is a non-imidazole histamine H4 receptor agonist; binds to rat H4 receptor with a pKi of 7.46.
  • 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-B0781
    Promethazine hydrochloride Antagonist 99.36%
    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-30234A
    Clemizole hydrochloride Antagonist 99.70%
    Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication.
  • HY-A0015
    Bepotastine Beslilate Antagonist 99.36%
    Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.
  • 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-B0539
    Desloratadine Antagonist 99.91%
    Desloratadine(Sch34117) is a potent antagonist for human histamine H1 receptor used to treat allergies.
  • 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-B0349
    Meclizine dihydrochloride Antagonist 99.81%
    Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness
  • HY-14447
    Bilastine Antagonist 99.95%
    Bilastine is a selective histamine H1 receptor antagonist used for treatment of allergic rhinoconjunctivitis and urticaria.
  • 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-B0377
    Famotidine Antagonist 99.26%
    Famotidine is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
  • 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-17043
    Loratadine Agonist 99.81%
    Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.