2. Signaling Pathways
  3. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  4. Histamine Receptor

Histamine Receptor

Histamine Receptor

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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 Isoform Specific Products:

Histamine Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-I0021
    Bepotastine
    		Antagonist 98.58%
    Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.
    Bepotastine
  • HY-A0129
    Histamine phosphate
    		Agonist 99.34%
    Histamine phosphate is the agonist for histamine receptor and a vasodilator. Histamine phosphate is an organic nitrogen compound that participates in local immune responses, regulates intestinal physiological functions, and acts as a neurotransmitter. Histamine phosphate affects p38 MAPK/Akt signaling pathway, exhibits antitumor, antioxidant and anti-inflammatory activities. Histamine phosphate can be used in the research of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma.
    Histamine phosphate
  • HY-B0462
    Azelastine hydrochloride
    		Antagonist 99.93%
    Azelastine hydrochloridem, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine hydrochloride can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2.
    Azelastine hydrochloride
  • HY-B1204S
    Histamine-α,α,β,β-d4 dihydrochloride
    		Activator ≥98.0%
    Histamine-α,α,β,β-d4 (dihydrochloride) is the deuterium labeled Histamine. 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.
    Histamine-α,α,β,β-d<sub>4</sub> dihydrochloride
  • HY-111827
    S-1-Propenyl-L-cysteine
    		99.91%
    S-1-Propenyl-L-cysteine is a stereoisomer of S-allyl-l-cysteine, extracted from garlic, with immunomodulatory effects and reduces blood pressure in a hypertensive animal model. S-1-Propenyl-L-cysteine exhibits antioxidative efficacy through a NO-dependent BACH1 signaling pathway. S-1-Propenyl-L-cysteine is orally active.
    S-1-Propenyl-L-cysteine
  • HY-30234A
    Clemizole hydrochloride
    		Antagonist 99.99%
    Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole hydrochloride is an inhibitor of TRPC5 channel. The IC50 of Clemizole hydrochloride for RNA binding by NS4B is 24 nM, whereas its EC50 for viral replication is 8 μM.
    Clemizole hydrochloride
  • HY-B0640
    Epinastine
    		Antagonist ≥98.0%
    Epinastine (WAL801) is a selective and orally active histamine H1 receptor antagonist, CD96/PVR inhibitor and mast cell stabilizer. Epinastine has high affinity for neuronal octopamine receptors in locusts (Ki = 2 nM) and honeybees (Ki = 1.1 nM). Epinastine hydrochloride inhibits TARC, IL-8, and IL-4. Epinastine activates anti-colon cancer immunity and inhibits Substance P (HY-P0201)-induced scratching behavior and increased vascular permeability. Epinastine can be used in the research of allergic diseases.
    Epinastine
  • HY-B0478A
    Trazodone
    		Antagonist 99.84%
    Trazodone (AF-1161 free base) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone has anti-depressant and anti-insomnious activity. Trazodone exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.
    Trazodone
  • HY-B1296
    Promethazine
    		Antagonist 99.67%
    Promethazine is an orally active histamine receptor antagonist. Promethazine is first-generation antihistamine of the phenothiazine family, shows strong sedative and weak antipsychotic effects.
    Promethazine
  • HY-B1693
    Levomepromazine
    		Antagonist 99.98%
    Levomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.
    Levomepromazine
  • HY-B0478
    Trazodone hydrochloride
    		Antagonist 99.60%
    Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.
    Trazodone hydrochloride
  • HY-B1794
    Thiethylperazine
    		Antagonist 99.91%
    Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects.
    Thiethylperazine
  • HY-B0281A
    Ranitidine hydrochloride
    		Antagonist 99.86%
    Ranitidine hydrochloride is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine hydrochloride antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine hydrochloride inhibits breast tumor development and spread in mice.
    Ranitidine hydrochloride
  • HY-19705B
    Adriforant hydrochloride
    		Antagonist ≥98.0%
    Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
    Adriforant hydrochloride
  • HY-B0693
    Ranitidine
    		Antagonist ≥99.0%
    Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine inhibits breast tumor development and spread in mice.
    Ranitidine
  • HY-13448
    Nedocromil
    		Inhibitor 98.75%
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
    Nedocromil
  • HY-A0015
    Bepotastine besilate
    		Antagonist 99.77%
    Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.
    Bepotastine besilate
  • HY-B0548A
    Hydroxyzine dihydrochloride
    		Antagonist 99.81%
    Hydroxyzine dihydrochloride, a benzodiazepine antihistamine agent, acts as a orally active histamine?H1-receptor and serotonin antagonist. Hydroxyzine dihydrochloride has anxiolytic effect and can be used forthe research of generalised anxiety disorder.
    Hydroxyzine dihydrochloride
  • HY-112175
    N-Acetylhistamine
    		99.98%
    N-Acetylhistamine is a histamine metabolite. N-acetylhistamine can be used as a potential biomarker of histidine metabolism for anaphylactoid reactions.
    N-Acetylhistamine
  • HY-14111
    GSK189254A
    		Antagonist 98.59%
    GSK189254A (GSK189254 free base) 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.
    GSK189254A
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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