Histamine Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
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

Isoform-specific Inhibitors

Histamine Receptor Inhibitors (64)
New Histamine Receptor Products

Catalog No.	Information	Product Use Citations	Product Validations
S4199^New	Antazoline HCl Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.
S1291	Cetirizine DiHCl Cetirizine DiHCl is an antihistamine.	J Allergy Clin Immunol, 2016, 10.1016/j.jaci.2016.03.028	Body temperatures of pretreated mice during IgG1-induced PSA in FcγRIIB-/- (n=6 per group) or WT (n=4 per group) mice.
S3208	Fexofenadine HCl Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.	Sci Rep, 2016, 10.1038/srep25694
S4253	Epinastine HCl Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
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.
S3052	Rupatadine Fumarate Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with K_i of 550 nM and 102 nM, respectively.
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.
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.
S2308	Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
S4696	CarbinoxaMine Maleate Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.
S4240	Doxylamine Succinate Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.
S3176	Betahistine 2HCl Betahistine is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
S1847	Clemastine Fumarate Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.	Neurosci Bull, 2015, 31(5):617-25 Front Cell Neurosci, 2018, 12:412	(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.
S1245	Latrepirdine 2HCl 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.
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.
S3037	Bepotastine Besilate Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
S1382	Mianserin HCl Mianserin is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.
S5926^New	Pitolisant hydrochloride 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.
S5649^New	Hydroxyzine pamoate 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.
S5662^New	Ranitidine 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.
S5670^New	Chloropyramine hydrochloride Chloropyramine hydrochloride is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.
S5656^New	Diphenylpyraline hydrochloride 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.
S5718^New	Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5659^New	Emedastine 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).
S5647^New	Emedastine Difumarate Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.
S5447^New	Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5479^New	Cloperastine hydrochloride Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
S5018^New	Mebhydrolin napadisylate Mebhydrolin Napadisylate is classified as an antihistamine drug classes used to treat allergies.
S4849^New	Levocetirizine Dihydrochloride Levocetirizine is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.
S2552	Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
S1801	Ranitidine Hydrochloride Ranitidine is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.
S1866	Diphenhydramine HCl Diphenhydramine HCl is a first-generation histamine H1 receptor antagonist, used in various allergic conditions such as rhinitis, urticaria and conjunctivitis.	Sci Rep, 2017, 7(1):8491
S4012	Desloratadine Desloratadine is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.
S1816	Chlorpheniramine Maleate Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) is an histamine H1 receptor antagonist with IC50 of 12 nM.
S2813	Ciproxifan Maleate 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.
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.
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.
S1845	Cimetidine Cimetidine, a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.
S2065	Lafutidine Lafutidine, a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
S1890	Nizatidine Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
S3146	Tripelennamine HCl Tripelennamine is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
S2044	Cyproheptadine HCl Cyproheptadine HCl is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.
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.	Nature, 2018, 560(7718):372-376	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.
S4262	Ebastine Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.
S2585	Brompheniramine hydrogen maleate Brompheniramine hydrogen maleate is a histamine H1 receptors antagonist.
S2905	JNJ-7777120 JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with K_i of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
S4008	Pemirolast potassium Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
S4139	Cyclizine 2HCl Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
S4625	Alcaftadine 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.
S4045	Pheniramine Maleate Pheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria.
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.
S8598	S 38093 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.
S3721	Bilastine Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
S3120	Doxepin HCl Doxepin is a tricyclic antidepressant formulated as a mixture of E-(trans) and Z-(cis) stereoisomers. It inhibits CYP2D6 activity in vivo.
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.
S4293	Promethazine HCl Promethazine HCl is a potent histamine H₁ receptor antagonist, used as a sedative and antiallergic medication.
S5619^New	Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S5498^New	Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S1357	Lidocaine Lidocaine is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.	Antiviral Res, 2016, 132:38-45
S3968	Histamine 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.
S4117	Histamine Phosphate Histamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.
S4118	Histamine 2HCl Histamine is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.

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Histamine Receptor

Signaling Pathway Map

Research Area

Isoform-specific Inhibitors