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-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-10121
    Asenapine
    		Antagonist 99.62%
    Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
    Asenapine
  • HY-14447
    Bilastine
    		Antagonist 99.91%
    Bilastine is an oral histamine H1-receptor antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system.
    Bilastine
  • HY-123205
    Oxatomide
    		Antagonist 99.56%
    Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
    Oxatomide
  • 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-B0426A
    Olopatadine hydrochloride
    		Inhibitor 99.71%
    Olopatadine hydrochloride (ALO4943A) is a histamine blocker used to treat allergic conjunctivitis.
    Olopatadine hydrochloride
  • HY-B0814
    Levocetirizine
    		Antagonist 99.41%
    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-A0027
    Fenspiride hydrochloride
    		Antagonist 99.11%
    Fenspiride, an orally active non-steroidal antiinflammatory agent, is an antagonist of H1-histamine receptor. Fenspiride inhibites phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4) and phosphodiesterase 5 (PDE5) activities with -log IC50 values of 3.44, 4.16 and approximately 3.8, respectively. Fenspiride can be used for the research of respiratory diseases.
    Fenspiride hydrochloride
  • HY-B0274A
    Chlorprothixene hydrochloride
    		Antagonist 99.91%
    Chlorprothixene hydrochloride 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 hydrochloride
  • HY-B1296
    Promethazine
    		Antagonist 99.61%
    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-103093
    Zotepine
    		Antagonist 99.85%
    Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo.
    Zotepine
  • HY-B0895
    Hydroxyzine pamoate
    		Antagonist 99.85%
    Hydroxyzine pamoate is a histamine receptor H1 antagonist, one of the salt forms of Hydroxyzine, soluble in dimethyl formamide and chloroform but insoluble in water and alcohol.
    Hydroxyzine pamoate
  • HY-B0693
    Ranitidine
    		Antagonist ≥99.0%
    Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion. Ranitidine is a weak inhibitor of CYP2C19 and CYP2C9.
    Ranitidine
  • HY-W010841
    Levocetirizine dihydrochloride
    		Antagonist 99.73%
    Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.
    Levocetirizine dihydrochloride
  • HY-B1165
    Cyproheptadine hydrochloride sesquihydrate
    		Antagonist 99.82%
    Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
    Cyproheptadine hydrochloride sesquihydrate
  • HY-107565
    2-Pyridylethylamine hydrochloride
    		Agonist 99.86%
    2-Pyridylethylamine is a histamine-1 (H1R) receptor agonist. 2-Pyridylethylamine can reduce the joint injury induced by formalin in rats. 2-Pyridylethylamine can be used to study the spinal cord release of neuropeptide (NPY) .
    2-Pyridylethylamine hydrochloride
  • HY-108411
    Emedastine
    		Antagonist 98.01%
    Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.
    Emedastine
  • HY-B0524
    Betahistine
    		Modulator 98.04%
    Betahistine is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine is used for the study of rheumatoid arthritis (RA).
    Betahistine
  • HY-B0640A
    Epinastine hydrochloride
    		Antagonist 99.73%
    Epinastine hydrochloride (WAL801 hydrochloride) is an antihistamine and mast cell stabilizer. Epinastine hydrochloride is a potent, selective and orally-active histamine H1 receptor antagonist. Epinastine hydrochloride also inhibits IL-8 release and has an antiallergic action.
    Epinastine hydrochloride
  • HY-A0075
    Decloxizine dihydrochloride
    		Antagonist 99.82%
    Decloxizine dihydrochloride(UCB-1402; NSC289116) is a histamine 1 receptor antagonist.
    Decloxizine dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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