Histamine Receptor

Signaling Pathway Map

Research Area

  • Inhibitory Selectivity
  • Solubility
Catalog No. Product Name Solubility(25°C)
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

Catalog No. Information Product Use Citations Product Validations

Antazoline HCl

Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.


Cetirizine DiHCl

Cetirizine DiHCl is an antihistamine.


Fexofenadine HCl

Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.


Epinastine HCl

Epinastine is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.


Olopatadine HCl

Olopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine.


Buclizine HCl

Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.


Rupatadine Fumarate

Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.


Ketotifen Fumarate

Ketotifen Fumarate is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer.


Azatadine dimaleate

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

Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.


Doxylamine Succinate

Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.


Betahistine 2HCl

Betahistine is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.


Clemastine Fumarate

Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.


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.



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 Besilate

Bepotastine is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.


Mianserin HCl

Mianserin is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.


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.


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.



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

Chloropyramine hydrochloride is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.


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.



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

Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.


Triprolidine Hydrochloride

Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.


Cloperastine hydrochloride

Cloperastine is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.


Mebhydrolin napadisylate

Mebhydrolin Napadisylate is classified as an antihistamine drug classes used to treat allergies.


Levocetirizine Dihydrochloride

Levocetirizine is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.


Azelastine HCl

Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.


Ranitidine Hydrochloride

Ranitidine is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.


Diphenhydramine HCl

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 Maleate

Chlorpheniramine (Chlorpheniramine maleate, Chlorphenamine) is an histamine H1 receptor antagonist with IC50 of 12 nM.


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.


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.



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 HCl

Tripelennamine is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.


Cyproheptadine HCl

Cyproheptadine HCl is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.


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.



Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.


Brompheniramine hydrogen maleate

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

Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.


Cyclizine 2HCl

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

Pheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria.


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.


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.



Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.


Doxepin HCl

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

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

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 Phosphate

Histamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.


Histamine 2HCl

Histamine is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.