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-100238
    Antihistamine-1
    		Inhibitor 99.45%
    Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
    Antihistamine-1
  • HY-12966
    Cetirizine methyl ester
    Cetirizine methyl ester is an impurity of Cetirizine (HY-17042). Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist.
    Cetirizine methyl ester
  • HY-107566
    Conessine
    		Antagonist 99.87%
    Conessine is an orally active and BBB-penetrable selective histamine H3 receptor antagonist. The pKi values of Conessine for rat and human H3 receptors are 7.61 and 8.27, respectively. Conessine is an inhibitor of the multidrug efflux pump system in Pseudomonas aeruginosa and can enhance the activity of antibiotics. Conessine has antimalarial activity. Conessine can also be used in the research of muscle atrophy.
    Conessine
  • HY-105542
    Niaprazine
    		Antagonist 99.67%
    Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research.
    Niaprazine
  • HY-112219A
    H3R antagonist 1 hydrochloride
    		Inhibitor 99.10%
    H3R antagonist 1 hydrochloride is a histamine receptor 3 (H3R) inverse agonist. H3R antagonist 1 hydrochloride increases the expression levels of myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes. H3R antagonist 1 hydrochloride can be used for the study of multiple sclerosis.
    H3R antagonist 1 hydrochloride
  • HY-15645
    H4R antagonist 2
    		Antagonist 98.92%
    H4R antagonist 2 (page 68), a Furo[3,2-d]pyrimidine derivative, is a potent H4R antagonist. H4R antagonist 2 can be used in research of rheumatoid arthritis.
    H4R antagonist 2
  • 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-101052
    HTMT dimaleate
    		Agonist 99.55%
    HTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 104 times more active than histamine in H2-mediated effects in natural suppressor cells.
    HTMT dimaleate
  • HY-B1589A
    Carbinoxamine maleate salt
    		Antagonist 99.81%
    Carbinoxamine maleate salt is a histamine H1 receptor antagonist.
    Carbinoxamine maleate salt
  • 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 (CO-1177) 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-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-101167
    Aminopotentidine
    		Antagonist 98.54%
    Aminopotentidine is a histamine H2 receptor antagonist with KB values of 220 nM and 280 nM for human and guinea pig H2 receptors, respectively. It can also serve as a precursor for the synthesis of [125I] iodo derivatives.
    Aminopotentidine
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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