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-B0157A
    Ketotifen fumarate
    		Inhibitor 99.92%
    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-10791
    Ritanserin
    		Inhibitor 99.68%
    Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
    Ritanserin
  • HY-B0781
    Promethazine hydrochloride
    		Antagonist 99.20%
    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-13508
    JNJ-7777120
    		Antagonist 99.85%
    JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory.
    JNJ-7777120
  • HY-B0674
    Ebastine
    		Antagonist 99.67%
    Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.
    Ebastine
  • HY-17042A
    Cetirizine dihydrochloride
    		Antagonist 99.53%
    Cetirizine dihydrochloride, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine dihydrochloride marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
    Cetirizine dihydrochloride
  • HY-12199B
    Pitolisant hydrochloride
    		Antagonist 99.96%
    Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
    Pitolisant hydrochloride
  • HY-B0286A
    Chlorpheniramine maleate
    		Antagonist 99.90%
    Chlorpheniramine maleate is a histamine H1 receptor antagonist with an IC50 of 12 nM.
    Chlorpheniramine maleate
  • HY-B0188A
    Mianserin hydrochloride
    		Inhibitor 99.87%
    Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
    Mianserin hydrochloride
  • HY-B0352
    Mirtazapine
    		Antagonist 99.94%
    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
  • HY-14270
    Lodoxamide
    		Inhibitor 98.07%
    Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
    Lodoxamide
  • HY-B1281
    Mepyramine maleate
    		Antagonist 99.93%
    Mepyramine maleate, a first generation antihistamine, is an antagonist of histamine H1 receptor, with Kds of 0.8 nM, 5200 nM and >3000 nM for H1, H2, and H3 receptor, respectively, and a pKd of 9.4 for H1 receptor.
    Mepyramine maleate
  • HY-111827
    S-1-Propenyl-L-cysteine
    		99.81%
    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-19705B
    Adriforant hydrochloride
    		Antagonist ≥98.0%
    Adriforant hydrochloride (PF-3893787 hydrochloride) is a novel histamine H4 receptor antagonist binding affinity (Ki=2.4 nM) and is also a functional (Ki=1.56 nM) antagonist.
    Adriforant hydrochloride
  • HY-B1204S
    Histamine-α,α,β,β-d4 dihydrochloride
    		Activator ≥98.0%
    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-A0129
    Histamine phosphate
    		Agonist 99.99%
    Histamine (phosphate) is a strong histamine receptor activator and vasodilator neuroagent, capable of activating nitric oxide synthase.
    Histamine phosphate
  • HY-B0303
    Diphenhydramine
    		Antagonist 99.08%
    Diphenhydramine is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB) .
    Diphenhydramine
  • HY-17042
    Cetirizine
    		Antagonist 99.51%
    Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
    Cetirizine
  • HY-W127758
    Alginic acid
    Alginic acid is a natural polysaccharide, which has been widely concerned and applied due to its excellent water solubility, film formation, biodegradability and biocompatibility. Alginic acid induces oxidative stress-mediated hormone secretion disorder, apoptosis and autophagy in mouse granulosa cells and ovaries. Alginic acid has an inhibitory effect on histamine release. Anti-anaphylactic and anti-inflammatory properties.
    Alginic acid
Cat. No. Product Name / Synonyms Application Reactivity
Histamine Receptor Isoform Comparison

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