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-B0539S
    Desloratadine-d4
    		Antagonist
    Desloratadine-d4 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities[1][2].
    Desloratadine-d<sub>4</sub>
  • HY-17043S
    Loratadine-d4
    		Agonist
    Loratadine-d4 is the deuterium labeled Loratadine. 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. Loratadine can inhibit immunologic release of inflammatory mediators.
    Loratadine-d<sub>4</sub>
  • HY-B0524AS
    Betahistine-d3 dihydrochloride
    		Modulator ≥99.0%
    Betahistine-d3 (dihydrochloride) is the deuterium labeled Betahistine dihydrochloride. Betahistine dihydrochloride is an orally active histamine H1 receptor agonist and a H3 receptor antagonist. Betahistine dihydrochloride is used for the study of rheumatoid arthritis (RA).
    Betahistine-d<sub>3</sub> dihydrochloride
  • HY-14289S
    Cimetidine-d3
    		Modulator
    Cimetidine-d3 is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity.
    Cimetidine-d<sub>3</sub>
  • HY-B0539S1
    Desloratadine-d9
    		Antagonist
    Desloratadine-d9 is the deuterium labeled Desloratadine. Desloratadine (Sch34117) is the orally active major metabolite of the nonsedating H1-antihistamine Loratadine. Desloratadine is a selective H1-receptor antagonist that has anti-allergic and anti-inflammatory activities.
    Desloratadine-d<sub>9</sub>
  • HY-B0814S
    Levocetirizine-d4 dihydrochloride
    		Antagonist
    Levocetirizine-d4 (dihydrochloride) is the deuterium labeled Levocetirizine. 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[1].
    Levocetirizine-d<sub>4</sub> dihydrochloride
  • HY-121356S1
    Carebastine-d5 Methyl Ester
    		Antagonist
    Carebastine-d5 Methyl Ester is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner. Carebastine suppresses the expression of macrophage migration inhibitory factor.
    Carebastine-d<sub>5</sub> Methyl Ester
  • HY-B0274AS
    Chlorprothixene-d6 hydrochloride
    		Antagonist
    Chlorprothixene-d6 hydrochloride is the deuterium labeled Chlorprothixene hydrochloride. 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-d<sub>6</sub> hydrochloride
  • HY-12532S
    Astemizole-d3
    Astemizole-d3 is the deuterium labeled Astemizole. 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.
    Astemizole-d<sub>3</sub>
  • HY-B1808S
    (E/Z)-Triprolidine-d8 hydrochloride
    (E/Z)-Triprolidine-d8 (hydrochloride) is the deuterium labeled (E/Z)-Triprolidine hydrochloride.
    (E/Z)-Triprolidine-d<sub>8</sub> hydrochloride
  • HY-B1296S
    Promethazine-d6 hydrochloride
    		Antagonist
    Promethazine-d6 (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is an orally active histamine receptor antagonist.
    Promethazine-d<sub>6</sub> hydrochloride
  • HY-121356S
    Carebastine-d5
    		Antagonist
    Carebastine-d5 is the deuterium labeled Carebastine. Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner. Carebastine suppresses the expression of macrophage migration inhibitory factor.
    Carebastine-d<sub>5</sub>
  • HY-139519S
    N-Desmethyl diphenhydramine-d3 hydrochloride
    		Inhibitor
    N-Desmethyl diphenhydramine-d3 (hydrochloride) is the deuterium labeled N-Desmethyl diphenhydramine hydrochloride.
    N-Desmethyl diphenhydramine-d<sub>3</sub> hydrochloride
  • HY-B0310S
    Nizatidine-d3
    		Antagonist 98.80%
    Nizatidine-d3 is the deuterium labeled Nizatidine. Nizatidine is a potent and orally active histamine H2 receptor antagonist, can be used for the research of stomach?and?intestines ulcers. Nizatidine works by decreasing the secretion of gastric?acid the stomach makes and prevent ulcers from coming back after they have healed in animal models.
    Nizatidine-d<sub>3</sub>
  • HY-B0286R
    Chlorpheniramine (Standard)
    		Antagonist
    Chlorpheniramine (Standard) is the analytical standard of Chlorpheniramine. This product is intended for research and analytical applications. Chlorpheniramine is a H1 antihistamines commonly used in allergic diseases research.
    Chlorpheniramine (Standard)
  • HY-B1510S
    Acrivastine-d7
    		Antagonist
    Acrivastine-d7 is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.
    Acrivastine-d<sub>7</sub>
  • HY-B0480A
    Brompheniramine
    		Antagonist
    Brompheniramine ((±)-Brompheniramine) is a potent and orally active antihistamine of the alkylamine class. Brompheniramine is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
    Brompheniramine
  • HY-B1317A
    Thonzylamine hydrochloride
    		Antagonist
    Thonzylamine hydrochloride is an orally active H1 histamine receptor antagonist with good antihistaminic and antianaphylactic properties. Thonzylamine hydrochloride can be used for the research of hypersensitivity diseases, nasal congestion, allergic conjunctivitis and other allergic diseases.
    Thonzylamine hydrochloride
  • HY-12191
    A-331440
    		Antagonist
    A-331440 is a potent and selective histamine H3 receptor antagonist that regulates neurotransmitter release by inhibiting presynaptic H3 receptors. In preclinical studies involving mice on a high-fat diet, A-331440 demonstrated dose-dependent effects on weight reduction and fat loss. At 5 mg/kg, it effectively decreased body weight comparable to dexfenfluramine, while at 15 mg/kg, it significantly reduced body fat and improved insulin tolerance, similar to mice on a low-fat diet. These findings suggest that A-331440 holds promise as an antiobesity agent by modulating histaminergic pathways involved in food intake and metabolic regulation.
    A-331440
  • HY-107563
    ROS 234
    		Antagonist
    ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access.
    ROS 234
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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