1. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  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 (171):

Cat. No. Product Name Effect Purity
  • HY-B1204
    Histamine Activator 99.96%
    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-B0298A
    Clemastine fumarate Antagonist 99.95%
    Clemastine (fumarate) (HS-592 (fumarate)) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
  • HY-17043
    Loratadine Agonist 99.60%
    Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity.
  • HY-B0801A
    Fexofenadine hydrochloride Inhibitor 99.61%
    Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years)[1].
  • HY-B1193
    Terfenadine Antagonist 99.93%
    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9[2].
  • HY-B1808A
    Triprolidine hydrochloride Antagonist
    Triprolidine is an oral active, first-generation histamine H1-receptor antagonist. Triprolidine can be used for the research of allergic rhinitis. triprolidine exhibits spinal motor and sensory block in rats[1][2][3].
  • HY-B1557A
    Betazole dihydrochloride Agonist
    Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity[1][2][3].
  • HY-D0237
    Betahistine mesylate Modulator >98.0%
    Betahistine mesylate is an orally active histamine H1 receptor agonist and a H3 receptor antagonist[1]. Betahistine mesylate is used for the study of rheumatoid arthritis (RA)[3].
  • HY-N0054
    Osthole Inhibitor 99.90%
    Osthole is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity. Osthole also suppresses the secretion of HBV in cells.
  • HY-12199B
    Pitolisant hydrochloride Antagonist 99.67%
    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-B0377
    Famotidine Antagonist 98.17%
    Famotidine (MK-208) is a competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
  • HY-12532
    Astemizole Antagonist 99.68%
    Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects[1][2].
  • HY-17042A
    Cetirizine dihydrochloride Antagonist 99.17%
    Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response[1][2][3].
  • HY-A0077
    Perphenazine Inhibitor 99.90%
    Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
  • HY-B0303A
    Diphenhydramine hydrochloride Antagonist 99.04%
    Diphenhydramine hydrochloride, a histamine H1 antagonist used as an antiemetic, antitussive, for dermatoses and pruritus, for hypersensitivity reactions, as a hypnotic, an antiparkinson, and as an ingredient in common cold preparations.
  • HY-13511A
    Rupatadine Fumarate Antagonist 99.93%
    Rupatadine Fumarate (UR-12592 Fumarate) is a potent dual PAF/H1 antagonist with Ki of 0.55/0.1 μM(rabbit platelet membranes/guinea pig cerebellum membranes)[1][2][3].
  • HY-14270
    Lodoxamide Inhibitor 99.71%
    Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
  • HY-B0188A
    Mianserin hydrochloride Inhibitor 99.85%
    Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
  • HY-B0674
    Ebastine Antagonist 99.96%
    Ebastine(LAS-W 090;RP64305) is a long-acting and selective H1-histamine receptor antagonist.