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-B1204S
    Histamine-α,α,β,β-d4 dihydrochloride
    		Activator 99.71%
    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-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-B0286A
    Chlorpheniramine maleate
    		Antagonist 99.67%
    Chlorpheniramine maleate is a histamine H1 receptor antagonist with an IC50 of 12 nM.
    Chlorpheniramine maleate
  • HY-I0021
    Bepotastine
    		Antagonist 99.88%
    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-B0157A
    Ketotifen fumarate
    		Inhibitor 99.88%
    Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.
    Ketotifen fumarate
  • HY-12199
    Pitolisant
    		Inhibitor 99.73%
    Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
    Pitolisant
  • 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-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-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-12206
    Thioperamide
    		Antagonist 99.91%
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [3H]histamine release. Thioperamide inhibits [3H]histamine synthesis with a Ki of 31 nM.
    Thioperamide
  • 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-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-B0286
    Chlorpheniramine
    		Antagonist 99.86%
    Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research.
    Chlorpheniramine
  • HY-B0548A
    Hydroxyzine dihydrochloride
    		Antagonist 99.59%
    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-B0814
    Levocetirizine
    		Antagonist 98.98%
    Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
    Levocetirizine
  • 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-17039
    Alcaftadine
    		Antagonist 98.37%
    Alcaftadine (R89674) is a histamine H1 receptor antagonist, which is used to prevent eye irritation brought on by allergic conjunctivitis. Alcaftadine is a broad-spectrum antihistamine displaying a high affinity for histamine H1 and H2 receptors and a lower affinity for H4 receptors. Alcaftadine also exhibits modulatory action on immune cell recruitment and mast cell stabilizing effects.
    Alcaftadine
  • 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-B0781
    Promethazine hydrochloride
    		Antagonist 99.85%
    Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.
    Promethazine hydrochloride
  • HY-B0274
    Chlorprothixene
    		Antagonist 99.87%
    Chlorprothixene is a dopamine and histamine receptors antagonist with Kis of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.
    Chlorprothixene
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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