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-B0352R
    Mirtazapine (Standard)
    		Antagonist 99.95%
    Mirtazapine (Standard) is the analytical standard of Mirtazapine. This product is intended for research and analytical applications. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
    Mirtazapine (Standard)
  • HY-100999
    (R)-(-)-α-Methylhistamine dihydrobromide
    		Agonist ≥98.0%
    (R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats.
    (R)-(-)-α-Methylhistamine dihydrobromide
  • HY-A0015A
    (Rac)-Bepotastine besilate
    		Inhibitor 99.52%
    (Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. 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.
    (Rac)-Bepotastine besilate
  • HY-15540
    Metiamide
    		Antagonist 98.08%
    Metiamide (SK&F 92058) is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide.
    Metiamide
  • HY-101179
    Tesmilifene fumarate
    		Antagonist 99.85%
    Tesmilifene fumarate (DPPE fumarate), an H1C receptor antagonist, potentiates a wide range of cytotoxics and even to offer some protection of normal cells.
    Tesmilifene fumarate
  • HY-158337
    Nesosteine
    		Inhibitor
    Nesosteine is a bronchitis inhibitor that improves the rheology and production of airway bronchial mucus in rabbits. Nesosteine significantly reduced the viscosity of airway bronchial mucus in animals with sulfuric acid nebulized bronchitis and increased mucus production in healthy animals. Nesosteine is more active than mucus-regulating drugs such as Sobrerol, N-acetylcysteine, bromhexine, ambroxol, S-carboxymethylcysteine, and mercaptoalanine. Nesosteine also reduced the content of total proteins in airway bronchial mucus, such as albumin, α1, α2, β, and γ mucins.
    Nesosteine
  • HY-19010A
    BMY-25368 hydrochloride
    		Antagonist
    BMY-25368 hydrochloride is a histamine H2 receptor antagonist that acts as a gastric acid secretion inhibitor. BMY-25368 hydrochloride competitively antagonizes gastric secretion stimulated by histamine and also antagonizes gastric secretion stimulated by Pentagastrin (HY-A0261), Bethanechol (HY-B0406), and food.
    BMY-25368 hydrochloride
  • HY-109968
    Irdabisant
    		Antagonist 99.38%
    Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment.
    Irdabisant
  • HY-145106
    Histamine H4 receptor antagonist-1
    		Antagonist 99.57%
    Histamine H4 receptor antagonist-1 is an antagonist of histamine H4 receptor extracted from patent WO2010108059A1 compound 60.
    Histamine H4 receptor antagonist-1
  • HY-117829
    UNC9994
    		Antagonist 98.06%
    UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
    UNC9994
  • HY-13218
    Acitazanolast
    		Inhibitor 98.70%
    Acitazanolast is an orally active antiallergic agent, can inhibit histamine release. Acitazanolast can be used in study of type I anaphylaxis (immediate) caused by IgE antibodies.
    Acitazanolast
  • HY-136338
    Cimetidine sulfoxide
    		Antagonist
    Cimetidine sulfoxide (Cimetidine sulphoxide) is a sulfoxide metabolite of Cimetidine. Cimetidine is a histamine H2-receptor antagonist. Cimetidine has the potential for peptic ulcer disease and upper gastrointestinal haemorrhage treatment.
    Cimetidine sulfoxide
  • HY-112067A
    Chlorcyclizine hydrochloride
    		Antagonist 99.77%
    Chlorcyclizine hydrochloride is a histamine H1 antagonist.
    Chlorcyclizine hydrochloride
  • HY-14880B
    Bavisant dihydrochloride hydrate
    		Antagonist 99.26%
    Bavisant dihydrochloride hydrate (JNJ31001074AAC) is an orally active, potent, brain-penetrating and highly selective antagonist of the histamine H3 receptor. Bavisant dihydrochloride hydrate can be used for attention-deficit hyperactivity disorder (ADHD) research.
    Bavisant dihydrochloride hydrate
  • HY-B0157AS
    Ketotifen-d3 fumarate
    		Inhibitor 99.23%
    Ketotifen-d3 (fumarate) is the deuterium labeled Ketotifen fumarate. Ketotifen (HC 20511) fumarate is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks[1][2].
    Ketotifen-d<sub>3</sub> fumarate
  • HY-17610A
    Enerisant hydrochloride
    		Antagonist 98.72%
    Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively.
    Enerisant hydrochloride
  • HY-19489S1
    (Rac)-Levomepromazine-d3 hydrochloride
    		Antagonist
    (Rac)-Levomepromazine-d3 (hydrochloride) is a labelled racemic Methotrimeprazine, which is a phenothiazine which has antagonist actions at multiple neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin and histamine receptors[1][2].
    (Rac)-Levomepromazine-d<sub>3</sub> hydrochloride
  • HY-128656
    LML134
    		Agonist 99.43%
    LML134 (compound 18b) is an orally active and high selective Histamine 3 receptor (H3R) inverse agonist with Kis of 0.3 nM and 12 nM for hH3R cAMP and hH3R bdg. LML134 penetrates the brain rapidly, leading to high H3R occupancy, and disengages its target with a fast kinetic profile. LML134 has the potential for excessive sleep disorders.
    LML134
  • HY-16344
    Nedocromil sodium
    		Inhibitor
    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
    Nedocromil sodium
  • HY-12537
    Peptide 401
    		Antagonist 98.26%
    Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
    Peptide 401
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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