Histamine Receptor

Histamine Receptor Inhibitors | Agonists | Antagonists (41)


Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1847 Clemastine Fumarate Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
S1358 Loratadine Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
S2552 Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
S1382 Mianserin HCl Mianserin is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.
S1801 Ranitidine Ranitidine is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.
S1245 Latrepirdine Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.
S3037 Bepotastine Besilate Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
S1291 Cetirizine DiHCl Cetirizine DiHCl is an antihistamine.
  • J Allergy Clin Immunol, 2016, 10.1016/j.jaci.2016.03.028
S1866 Diphenhydramine HCl Diphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis.
S1986 Meclizine 2HCl Meclizine is a histamine H1 receptor antagonist used to treat nausea and motion sickness, has anti-histamine, anti-muscarinic and anti-oxidative phosphorylation properties, also an agonist ligand for mCAR (constitutive androstane receptor) and an inverse agonist for hCAR.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2813 Ciproxifan Ciproxifan is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.
S2107 Mizolastine Mizolastine is a histamine H1-receptor antagonist with IC50 of 47 nM used in the treatment of hay fever (seasonal allergic rhinitis), hives and other allergic reactions.
S1816 Chlorpheniramine Maleate Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) is an histamine H1 receptor antagonist with IC50 of 12 nM.
S4012 Desloratadine Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.
S3208 Fexofenadine HCl Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.
  • Sci Rep, 2016, 10.1038/srep25694
S1890 Nizatidine Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
S1845 Cimetidine Cimetidine, a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.
S4253 Epinastine HCl Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
S2065 Lafutidine Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
S3146 Tripelennamine HCl Tripelennamine is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S1357 Lidocaine Lidocaine is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
  • Antiviral Res, 2016, 132:38-45
S2494 Olopatadine HCl Olopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine.
S4140 Buclizine HCl Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
S2585 Brompheniramine hydrogen maleate Brompheniramine hydrogen maleate is a histamine H1 receptors antagonist.
S4262 Ebastine Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.
S2024 Ketotifen Fumarate Ketotifen Fumarate is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer.
S3186 Azatadine dimaleate Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
S2905 JNJ-7777120 JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
S4026 Hydroxyzine 2HCl Hydroxyzine is a histamine H1-receptor antagonist, inhibits binding of [3H]pyrilamine/[3H]desloratadine to human histamine H1 receptor with IC50 of 10 nM/19 nM.
S3052 Rupatadine Fumarate Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S2044 Cyproheptadine HCl Cyproheptadine HCl is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.
S2078 Famotidine Famotidine is a histamine H2–receptor antagonist with IC50 of 0.6 mM, commonly used to treat heartburn, GERD, ulcers, and other digestive conditions.
S4118 Histamine 2HCl Histamine is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.
S4131 Levodropropizine Levodropropizine possess anti-allergic and inhibits histamine receptor, reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex.
S4117 Histamine Phosphate Histamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.
S4240 Doxylamine Succinate Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.
S1880 Roxatidine Acetate HCl Roxatidine Acetate HCl is a specific and competitive histamin H2-receptor antagonist, with IC50 of 3.2 μM, inhibits gastric acid secretion and ulcer formation.
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
S3176 Betahistine 2HCl Betahistine is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
S4008 Pemirolast potassium Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
Cat.No. Product Name Information Product Use Citation Customer Product Validation
S4139 Cyclizine 2HCl Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.

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Cat.No. Product Name Solubility (25°C)
Water DMSO Ethanol
S1847 Clemastine Fumarate <1 mg/mL 35 mg/mL <1 mg/mL
S1358 Loratadine <1 mg/mL 17 mg/mL 77 mg/mL
S2552 Azelastine HCl 35 mg/mL 84 mg/mL 84 mg/mL
S1382 Mianserin HCl 30 mg/mL 60 mg/mL 21 mg/mL
S1801 Ranitidine 70 mg/mL 70 mg/mL <1 mg/mL
S1245 Latrepirdine <1 mg/mL 24 mg/mL 13 mg/mL
S3037 Bepotastine Besilate <1 mg/mL 109 mg/mL <1 mg/mL
S1291 Cetirizine DiHCl 92 mg/mL 92 mg/mL <1 mg/mL
S1866 Diphenhydramine HCl 58 mg/mL 58 mg/mL 58 mg/mL
S1986 Meclizine 2HCl <1 mg/mL 4 mg/mL <1 mg/mL
S2813 Ciproxifan 1 mg/mL 54 mg/mL 54 mg/mL
S2107 Mizolastine <1 mg/mL <1 mg/mL <1 mg/mL
S1816 Chlorpheniramine Maleate 78 mg/mL 78 mg/mL 78 mg/mL
S4012 Desloratadine <1 mg/mL 26 mg/mL 62 mg/mL
S3208 Fexofenadine HCl 2 mg/mL 107 mg/mL 107 mg/mL
S1890 Nizatidine 28 mg/mL 66 mg/mL 18 mg/mL
S1845 Cimetidine <1 mg/mL 51 mg/mL 3 mg/mL
S4253 Epinastine HCl 57 mg/mL 57 mg/mL 57 mg/mL
S2065 Lafutidine <1 mg/mL 86 mg/mL 13 mg/mL
S3146 Tripelennamine HCl 58 mg/mL 2 mg/mL 1 mg/mL
S1357 Lidocaine 9 mg/mL 47 mg/mL 47 mg/mL
S2494 Olopatadine HCl 13 mg/mL 75 mg/mL 8 mg/mL
S4140 Buclizine HCl <1 mg/mL 0.2 mg/mL <1 mg/mL
S2585 Brompheniramine hydrogen maleate 46 mg/mL 87 mg/mL 18 mg/mL
S4262 Ebastine <1 mg/mL 4 mg/mL 11 mg/mL
S2024 Ketotifen Fumarate <1 mg/mL 8 mg/mL <1 mg/mL
S3186 Azatadine dimaleate 105 mg/mL 105 mg/mL <1 mg/mL
S2905 JNJ-7777120 <1 mg/mL 56 mg/mL 8 mg/mL
S4026 Hydroxyzine 2HCl 90 mg/mL 90 mg/mL 15 mg/mL
S3052 Rupatadine Fumarate <1 mg/mL 9 mg/mL 13 mg/mL
S2044 Cyproheptadine HCl <1 mg/mL 65 mg/mL 20 mg/mL
S2078 Famotidine <1 mg/mL 67 mg/mL <1 mg/mL
S4118 Histamine 2HCl 37 mg/mL 3 mg/mL <1 mg/mL
S4131 Levodropropizine 15 mg/mL 47 mg/mL 47 mg/mL
S4117 Histamine Phosphate 42 mg/mL <1 mg/mL <1 mg/mL
S4240 Doxylamine Succinate 78 mg/mL 78 mg/mL 78 mg/mL
S1880 Roxatidine Acetate HCl 77 mg/mL 77 mg/mL 12 mg/mL
S2308 Hesperetin <1 mg/mL 60 mg/mL <1 mg/mL
S3176 Betahistine 2HCl 38 mg/mL 38 mg/mL 1 mg/mL
S4008 Pemirolast potassium 53 mg/mL <1 mg/mL <1 mg/mL
S4139 Cyclizine 2HCl 68 mg/mL 7 mg/mL <1 mg/mL
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