- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S4199||Antazoline HCl||14 mg/mL||40 mg/mL||4 mg/mL|
|S1291||Cetirizine DiHCl||92 mg/mL||92 mg/mL||<1 mg/mL|
|S3208||Fexofenadine HCl||2 mg/mL||107 mg/mL||107 mg/mL|
|S4253||Epinastine HCl||57 mg/mL||57 mg/mL||57 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|
|S3052||Rupatadine Fumarate||<1 mg/mL||9 mg/mL||13 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|
|S4131||Levodropropizine||15 mg/mL||47 mg/mL||47 mg/mL|
|S2308||Hesperetin||<1 mg/mL||60 mg/mL||<1 mg/mL|
|S4696||CarbinoxaMine Maleate||81 mg/mL||81 mg/mL||81 mg/mL|
|S4240||Doxylamine Succinate||78 mg/mL||78 mg/mL||78 mg/mL|
|S3176||Betahistine 2HCl||38 mg/mL||38 mg/mL||1 mg/mL|
|S1847||Clemastine Fumarate||<1 mg/mL||35 mg/mL||<1 mg/mL|
|S1245||Latrepirdine 2HCl||<1 mg/mL||24 mg/mL||13 mg/mL|
|S1358||Loratadine||<1 mg/mL||17 mg/mL||76 mg/mL|
|S3037||Bepotastine Besilate||<1 mg/mL||109 mg/mL||<1 mg/mL|
|S1382||Mianserin HCl||30 mg/mL||60 mg/mL||21 mg/mL|
|S5926||Pitolisant hydrochloride||66 mg/mL||66 mg/mL||66 mg/mL|
|S5649||Hydroxyzine pamoate||-1 mg/mL||100 mg/mL||-1 mg/mL|
|S5662||Ranitidine||-1 mg/mL||63 mg/mL||-1 mg/mL|
|S5670||Chloropyramine hydrochloride||-1 mg/mL||65 mg/mL||-1 mg/mL|
|S5656||Diphenylpyraline hydrochloride||-1 mg/mL||63 mg/mL||-1 mg/mL|
|S5718||Acrivastine||-1 mg/mL||10 mg/mL||-1 mg/mL|
|S5447||Triprolidine Hydrochloride||-1 mg/mL||62 mg/mL||-1 mg/mL|
|S5479||Cloperastine hydrochloride||-1 mg/mL||73 mg/mL||-1 mg/mL|
|S5018||Mebhydrolin napadisylate||-1 mg/mL||8 mg/mL||-1 mg/mL|
|S4849||Levocetirizine Dihydrochloride||92 mg/mL||92 mg/mL||7 mg/mL|
|S2552||Azelastine HCl||35 mg/mL||28 mg/mL||42 mg/mL|
|S1801||Ranitidine Hydrochloride||70 mg/mL||70 mg/mL||<1 mg/mL|
|S1866||Diphenhydramine HCl||58 mg/mL||58 mg/mL||58 mg/mL|
|S4012||Desloratadine||<1 mg/mL||26 mg/mL||62 mg/mL|
|S1816||Chlorpheniramine Maleate||78 mg/mL||78 mg/mL||78 mg/mL|
|S2813||Ciproxifan Maleate||1 mg/mL||54 mg/mL||54 mg/mL|
|S1986||Meclizine 2HCl||<1 mg/mL||4 mg/mL||<1 mg/mL|
|S2107||Mizolastine||<1 mg/mL||<1 mg/mL||<1 mg/mL|
|S1845||Cimetidine||<1 mg/mL||51 mg/mL||3 mg/mL|
|S2065||Lafutidine||<1 mg/mL||86 mg/mL||13 mg/mL|
|S1890||Nizatidine||28 mg/mL||66 mg/mL||18 mg/mL|
|S3146||Tripelennamine HCl||58 mg/mL||2 mg/mL||1 mg/mL|
|S2044||Cyproheptadine HCl||<1 mg/mL||65 mg/mL||20 mg/mL|
|S4026||Hydroxyzine 2HCl||90 mg/mL||90 mg/mL||15 mg/mL|
|S4262||Ebastine||<1 mg/mL||4 mg/mL||11 mg/mL|
|S2585||Brompheniramine hydrogen maleate||46 mg/mL||87 mg/mL||18 mg/mL|
|S2905||JNJ-7777120||<1 mg/mL||56 mg/mL||8 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|
|S4625||Alcaftadine||<1 mg/mL||28 mg/mL||61 mg/mL|
|S4045||Pheniramine Maleate||71 mg/mL||71 mg/mL||71 mg/mL|
|S1880||Roxatidine Acetate HCl||77 mg/mL||77 mg/mL||12 mg/mL|
|S8598||S 38093||<1 mg/mL||57 mg/mL||57 mg/mL|
|S3721||Bilastine||<1 mg/mL||1 mg/mL||<1 mg/mL|
|S3120||Doxepin HCl||63 mg/mL||63 mg/mL||63 mg/mL|
|S2078||Famotidine||<1 mg/mL||67 mg/mL||<1 mg/mL|
|S4293||Promethazine HCl||64 mg/mL||64 mg/mL||34 mg/mL|
|S5498||Betahistine mesylate||-1 mg/mL||65 mg/mL||-1 mg/mL|
|S1357||Lidocaine||9 mg/mL||47 mg/mL||47 mg/mL|
|S3968||Histamine||-1 mg/mL||22 mg/mL||-1 mg/mL|
|S4117||Histamine Phosphate||42 mg/mL||<1 mg/mL||<1 mg/mL|
|S4118||Histamine 2HCl||37 mg/mL||3 mg/mL||<1 mg/mL|
- Histamine Receptor Inhibitors (64)
- New Histamine Receptor Products
|Catalog No.||Information||Product Use Citations||Product Validations|
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.
Cetirizine DiHCl is an antihistamine.
Body temperatures of pretreated mice during IgG1-induced PSA in FcγRIIB-/- (n=6 per group) or WT (n=4 per group) mice.
Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.
Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
Olopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine.
Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.
Ketotifen Fumarate is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer.
Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
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.
Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.
Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.
Betahistine is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.
(B,C) Analysis indicates the total distance was unchanged between cuprizone-exposed mice with or without clemastine treatment (B), but the distance in the central field decreased upon 6-week exposure to cuprizone, while clemastine gradually rescued the behavioral change (C). *P <0.05, n = 10 animals/group.
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.
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.
Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
Mianserin is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.
Pitolisant acts as a high-affinity competitive antagonist (Ki=0.16 nM) and as an inverse agonist (EC50=1.5 nM) at the human histamine H3 receptor subtype.
Hydroxyzine Pamoate is the pamoate salt form of hydroxyzine, a synthetic piperazine histamine H1-receptor antagonist with anti-allergic, antispasmodic, sedative, anti-emetic and anti-anxiety properties.
Ranitidine is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid released by cells of the stomach.
Chloropyramine hydrochloride is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.
Diphenylpyraline hydrochloride is the hydrochloride salt form of diphenylpyraline, which is an antihistamine used in the treatment of allergic rhinitis, hay fever, and allergic skin disorders.
Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
Emedastine is a potent, high affinity histamine H1-receptor-selective antagonist with Ki of 1.3 ±0.1 nM for H1-receptors while considerably weaker at H2- (K1 = 49,067 ± 11,113 nM) and H3-receptors (Ki = 12,430 ± 1,282 nM).
Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.
Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
Mebhydrolin Napadisylate is classified as an antihistamine drug classes used to treat allergies.
Levocetirizine is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.
Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Ranitidine is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.
Diphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis.
Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.
Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) is an histamine H1 receptor antagonist with IC50 of 12 nM.
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.
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.
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.
Cimetidine, a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.
Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
Tripelennamine is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
Cyproheptadine HCl is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.
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.
a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM. b, Quantification of sterol levels in OPCs treated with the indicated previously reported enhancers of oligodendrocyte formation (n = 2 wells per condition except DMSO, n = 6). Representative of two independent experiments; for concentrations, see Extended Data Fig. 6g. c, Quantification of EBP enzymatic activity in a biochemical assay. All treatments 10 μM. n = 3 independent enzymatic assays, except DMSO, n = 5. Bars indicate mean; error bars indicate s.d. Sigma H127, p-fluorohexahydro-sila-difenidol.
Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.
Brompheniramine hydrogen maleate is a histamine H1 receptors antagonist.
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.
Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
Alcaftadine is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor.
Pheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria.
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.
S 38093 is a histamine H3 antagonist/inverse agonist with a moderate affinity for rat, mouse and human H3 receptors (Ki = 8.8, 1.44 and 1.2 μM, respectively) and no affinity for other histaminergic receptors.
Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
Doxepin is a tricyclic antidepressant formulated as a mixture of E-(trans) and Z-(cis) stereoisomers. It inhibits CYP2D6 activity in vivo.
Famotidine is a histamine H2–receptor antagonist with IC50 of 0.6 mM, commonly used to treat heartburn, GERD, ulcers, and other digestive conditions.
Promethazine HCl is a potent histamine H1 receptor antagonist, used as a sedative and antiallergic medication.
Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
Lidocaine is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
Histamine, an organic nitrogenous compound, is involved in local immune responses regulating physiological function in the gut and acting as a neurotransmitter for the brain, spinal cord, and uterus. It is a potent H1 and H2 receptor agonist.
Histamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.
Histamine is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.