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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B0274
    Chlorprothixene
    		Antagonist 99.61%
    Chlorprothixene 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
  • 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-30234A
    Clemizole hydrochloride
    		Antagonist 99.99%
    Clemizole hydrochloride is an H1 histamine receptor antagonist, is found to substantially inhibit HCV replication. Clemizole hydrochloride is an inhibitor of TRPC5 channel. The IC50 of Clemizole hydrochloride for RNA binding by NS4B is 24 nM, whereas its EC50 for viral replication is 8 µM.
    Clemizole hydrochloride
  • HY-12199
    Pitolisant
    		Inhibitor
    Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
    Pitolisant
  • HY-W010841
    Levocetirizine dihydrochloride
    		Antagonist 99.56%
    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-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-13448
    Nedocromil
    		Inhibitor 98.02%
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
    Nedocromil
  • HY-10121
    Asenapine
    		Antagonist 99.93%
    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-14111
    GSK189254A
    		Antagonist 98.09%
    GSK189254A (GSK189254 free base) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively.
    GSK189254A
  • HY-107560
    4-Methylhistamine dihydrochloride
    		Agonist ≥99.0%
    4-Methylhistamine (dihydrochloride) is the potent agonist of histamine 4 receptor (H4R). 4-Methylhistamine (dihydrochloride) has the potential for the research of immune-related diseases such as cancer and autoimmune disorders.
    4-Methylhistamine dihydrochloride
  • 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-I0021
    Bepotastine
    		Antagonist 98.03%
    Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.
    Bepotastine
  • HY-B1557
    Betazole
    		Agonist
    Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active histamine H2 receptor agonist. Betazole induces gastric acid secretion and causes an immediate and significant increase in common bile duct pressure. Betazole is used as a diagnostic agent known as histalog for investigating gastric acid secretory capacity.
    Betazole
  • HY-B0538A
    Pemirolast potassium
    		Antagonist 99.93%
    Pemirolast potassium (TWT-8152) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
    Pemirolast potassium
  • HY-B1794
    Thiethylperazine
    		Antagonist 99.41%
    Thiethylperazine, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine has anti-emetic, antipsychotic and antimicrobial effects.
    Thiethylperazine
  • HY-W014941
    (R)-(-)-α-Methylhistamine dihydrochloride
    		Agonist 99.62%
    (R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM. (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats.
    (R)-(-)-α-Methylhistamine 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-B1062
    Dexchlorpheniramine maleate
    		Inhibitor ≥98.0%
    Dexchlorpheniramine maleate is an antihistamine, with anticholinergic properties, used to treat allergic conditions.
    Dexchlorpheniramine maleate
  • HY-B1090
    Cinnarizine
    		Inhibitor 99.63%
    Cinnarizine is an antihistamine and a calcium channel blocker, promote cerebral blood flow, used to treat cerebral apoplexy, post-trauma cerebral symptoms, and cerebral arteriosclerosis.
    Cinnarizine
  • HY-B0310
    Nizatidine
    		Antagonist 99.68%
    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
Cat. No. Product Name / Synonyms Application Reactivity