Histamine Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Histamine Receptor Products

All (74) Histamine Receptor Inhibitors (16) Histamine Receptor Antagonists (49) Histamine Receptor Agonists (9)

Catalog No.	Information	Product Use Citations	Product Validations
S1291	Cetirizine DiHCl Cetirizine DiHCl (UCB P071) is an antihistamine.	J Allergy Clin Immunol, 2017, 139(4):1253-1265 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 (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM.	Anticancer Res, 2019, 39(7):3767-3775 Sci Rep, 2016, 10.1038/srep25694
S4253	Epinastine HCl Epinastine (WAL-801CL) 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 (UCB-4445) 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.
S3183	Amitriptyline HCl Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA).	PLoS Pathog, 2020, 16;16(3):e1008341 Sci Rep, 2018, 8(1):15753
S3186	Azatadine dimaleate Azatadine (SCH10649) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.	Pharmaceuticals (Basel), 2019, 12(4)
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.
S5947	Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively.	Cancers (Basel), 2019, 11(12)
S4672	Dimenhydrinate Dimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness.
S2308	Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.	Carcinogenesis, 2020, 41(7):993-1004
S4696	CarbinoxaMine Maleate Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.	Am J Physiol Lung Cell Mol Physiol, 2019, 316(1):L20-L34 Anticancer Res, 2019, 39(7):3767-3775
S4240	Doxylamine Succinate Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.
S3176	Betahistine 2HCl Betahistine (PT-9) 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. Clemastine stimulates autophagy via mTOR pathway.	Nat Neurosci, 2020, 10.1038/s41593-020-0588-8 Acta Neuropathol, 2020, 140(5):715-736 Anticancer Res, 2019, 39(7):3767-3775	Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), p < 0.05, *p < 0.01).
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 (SCH29851) 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.	Adv Ther (Weinh), 2020, 2000034 Cell Syst, 2019, 8(2):97-108 Anticancer Res, 2019, 39(7):3767-3775
S3037	Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1382	Mianserin HCl Mianserin (ORG GB-94) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.	Immunity, 2019, 50(5):1163-1171
S0398^New	Astemizole Astemizole is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.
S2552	Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.	Anticancer Res, 2019, 39(7):3767-3775
S1801	Ranitidine Hydrochloride Ranitidine (AH19065) 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.	Int J Pharm, 2019, 560:294-305 Anticancer Res, 2019, 39(7):3767-3775 Sci Rep, 2017, 7(1):8491
S4012	Desloratadine Desloratadine (SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.	Anticancer Res, 2019, 39(7):3767-3775
S1816	Chlorpheniramine Maleate Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM.	Anticancer Res, 2019, 39(7):3767-3775
S2813	Ciproxifan Maleate Ciproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.	Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00548-6 Oncol Lett, 2018, 16(4):4921-4928
S1986	Meclizine 2HCl Meclizine (NSC 28728) 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.	Anticancer Res, 2019, 39(7):3767-3775
S2107	Mizolastine Mizolastine (SL 850324) 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 (SKF-92334), a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.	Anticancer Res, 2019, 39(7):3767-3775
S2065	Lafutidine Lafutidine (FRG-8813), 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.	Anticancer Res, 2019, 39(7):3767-3775
S3146	Tripelennamine HCl Tripelennamine (Pyribenzamine) 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.	Cell Rep, 2020, 21;31(3):107548 Vet Med Sci, 2020, 10.1002/vms3.336 Anticancer Res, 2019, 39(7):3767-3775
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.	Anticancer Res, 2019, 39(7):3767-3775 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.	Anticancer Res, 2019, 39(7):3767-3775
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.	Neuropharmacology, 2020, 168:108028 Mol Ther Methods Clin Dev, 2018, 11:83-91 Front Immunol, 2017, 8:1689
S4008	Pemirolast potassium Pemirolast potassium (BMY26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.	Front Microbiol, 2020, 10:2936 Anticancer Res, 2019, 39(7):3767-3775
S4849	Levocetirizine Dihydrochloride Levocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.	Anticancer Res, 2019, 39(7):3767-3775
S5670	Chloropyramine hydrochloride Chloropyramine hydrochloride (Halopyramine) is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.
S5659	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).
S4139	Cyclizine 2HCl Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
S5940	Bepotastine Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease.
S4625	Alcaftadine Alcaftadine (Lastacaft, R89674) 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.
S5479	Cloperastine hydrochloride Cloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
S5656	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.
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.
S5718	Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5447	Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5647	Emedastine Difumarate Emedastine Difumarate (Rapimine, Emedastine fumarate) is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.
S5018	Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies.
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.
S5926	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	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.	Anticancer Res, 2019, 39(7):3767-3775
S3721	Bilastine Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
S5662	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.	Anticancer Res, 2019, 39(7):3767-3775
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.
S4353	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S6435	Mequitazine Mequitazine is a histamine H1 antagonist which competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract.
S2078	Famotidine Famotidine (MK208) is a histamine H2–receptor antagonist with IC50 of 0.6 mM, commonly used to treat heartburn, GERD, ulcers, and other digestive conditions.	Anticancer Res, 2019, 39(7):3767-3775
S6469	Thonzylamine Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
S4293	Promethazine HCl Promethazine HCl is a potent histamine H₁ receptor antagonist, used as a sedative and antiallergic medication.	bioRxiv, 2020, 2020/9/20.4.7.30734 Anticancer Res, 2019, 39(7):3767-3775 Chem Biol Interact, 2019, 315:108888
S1357	Lidocaine Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.	Nat Biomed Eng, 2020, 4(3):286-297 J Cell Biochem, 2019, 120(10):16533-16542 Anticancer Res, 2019, 39(7):3767-3775
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.	Life Sci, 2019, 227:74-81
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.	Front Pharmacol, 2017, 8:667
S6612	Betazole Dihydrochloride Betazole Dihydrochloride is a histamine H2 agonist used clinically to test gastric secretory function.
S5498	Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S6569	VUF10460 VUF10460 is a histamine H4 receptor agonist.
S5619	Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S4382	Pyrilamine Maleate Pyrilamine Maleate (Mepyramine)is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.

Catalog No.	Information	Product Use Citations	Product Validations
S1291	Cetirizine DiHCl Cetirizine DiHCl (UCB P071) is an antihistamine.	J Allergy Clin Immunol, 2017, 139(4):1253-1265 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 (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM.	Anticancer Res, 2019, 39(7):3767-3775 Sci Rep, 2016, 10.1038/srep25694
S4253	Epinastine HCl Epinastine (WAL-801CL) 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 (UCB-4445) 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.
S3183	Amitriptyline HCl Amitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA).	PLoS Pathog, 2020, 16;16(3):e1008341 Sci Rep, 2018, 8(1):15753
S3186	Azatadine dimaleate Azatadine (SCH10649) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.	Pharmaceuticals (Basel), 2019, 12(4)
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.
S5947	Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively.	Cancers (Basel), 2019, 11(12)
S4672	Dimenhydrinate Dimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness.
S2308	Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.	Carcinogenesis, 2020, 41(7):993-1004
S4696	CarbinoxaMine Maleate Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.	Am J Physiol Lung Cell Mol Physiol, 2019, 316(1):L20-L34 Anticancer Res, 2019, 39(7):3767-3775
S4240	Doxylamine Succinate Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.
S3176	Betahistine 2HCl Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.

Catalog No.	Information	Product Use Citations	Product Validations
S1847	Clemastine Fumarate Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.	Nat Neurosci, 2020, 10.1038/s41593-020-0588-8 Acta Neuropathol, 2020, 140(5):715-736 Anticancer Res, 2019, 39(7):3767-3775	Detection of P2X7 receptor and histamine receptor H1 (HRH1) in hippocampus and mPFC. (A–F) CUMS treatment upregulated the protein expression of the purinergic receptor P2X, ligand-gated ion channel 7 (P2X7R) in both hippocampus and mPFC subregions. In the meantime, continuous intraperitoneal administration of clemastine protected mice from stress-induced upregulation of P2X7R in the hippocampus rather than mPFC. There is no statistical alteration of HRH1 expression in both subfields of hippocampus and mPFC, even when the mice were subjected to stress stimulation or clemastine injection (n = 4 for (A–F), p < 0.05, *p < 0.01).
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 (SCH29851) 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.	Adv Ther (Weinh), 2020, 2000034 Cell Syst, 2019, 8(2):97-108 Anticancer Res, 2019, 39(7):3767-3775
S3037	Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00420-z Hum Cell, 2020, 10.1007/s13577-020-00425-8
S1382	Mianserin HCl Mianserin (ORG GB-94) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.	Immunity, 2019, 50(5):1163-1171
S0398^New	Astemizole Astemizole is a histamine H1-receptor antagonist with IC50 of 4.7 nM. Astemizole is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. Astemizole has antineoplastic and antipruritic effects.
S2552	Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.	Anticancer Res, 2019, 39(7):3767-3775
S1801	Ranitidine Hydrochloride Ranitidine (AH19065) 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.	Int J Pharm, 2019, 560:294-305 Anticancer Res, 2019, 39(7):3767-3775 Sci Rep, 2017, 7(1):8491
S4012	Desloratadine Desloratadine (SCH-34117, NSC 675447) is a potent antagonist for human histamine H1 receptor with IC50 of 51 nM.	Anticancer Res, 2019, 39(7):3767-3775
S1816	Chlorpheniramine Maleate Chlorpheniramine Maleate (Chlorpheniramine maleate, Chlorphenamine, NCI-C55265) is an histamine H1 receptor antagonist with IC50 of 12 nM.	Anticancer Res, 2019, 39(7):3767-3775
S2813	Ciproxifan Maleate Ciproxifan (FUB 359) is a highly potent and selective histamin H3-receptor antagonist with IC50 of 9.2 nM, with low apparent affinity at other receptor subtypes.	Acta Pharmacol Sin, 2020, 10.1038/s41401-020-00548-6 Oncol Lett, 2018, 16(4):4921-4928
S1986	Meclizine 2HCl Meclizine (NSC 28728) 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.	Anticancer Res, 2019, 39(7):3767-3775
S2107	Mizolastine Mizolastine (SL 850324) 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 (SKF-92334), a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.	Anticancer Res, 2019, 39(7):3767-3775
S2065	Lafutidine Lafutidine (FRG-8813), 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.	Anticancer Res, 2019, 39(7):3767-3775
S3146	Tripelennamine HCl Tripelennamine (Pyribenzamine) 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.	Cell Rep, 2020, 21;31(3):107548 Vet Med Sci, 2020, 10.1002/vms3.336 Anticancer Res, 2019, 39(7):3767-3775
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.	Anticancer Res, 2019, 39(7):3767-3775 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.	Anticancer Res, 2019, 39(7):3767-3775
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.	Neuropharmacology, 2020, 168:108028 Mol Ther Methods Clin Dev, 2018, 11:83-91 Front Immunol, 2017, 8:1689
S4008	Pemirolast potassium Pemirolast potassium (BMY26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.	Front Microbiol, 2020, 10:2936 Anticancer Res, 2019, 39(7):3767-3775
S4849	Levocetirizine Dihydrochloride Levocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.	Anticancer Res, 2019, 39(7):3767-3775
S5670	Chloropyramine hydrochloride Chloropyramine hydrochloride (Halopyramine) is a histamine receptor H1 antagonist and has anti-cholinergic, antispasmodic, and antiallergic effects.
S5659	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).
S4139	Cyclizine 2HCl Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
S5940	Bepotastine Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor that is indicated in allergic rhinitis, urticaria, and pruritus associated with skin disease.
S4625	Alcaftadine Alcaftadine (Lastacaft, R89674) 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.
S5479	Cloperastine hydrochloride Cloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
S5656	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.
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.
S5718	Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5447	Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5647	Emedastine Difumarate Emedastine Difumarate (Rapimine, Emedastine fumarate) is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity.
S5018	Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies.
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.
S5926	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	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.	Anticancer Res, 2019, 39(7):3767-3775
S3721	Bilastine Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
S5662	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.	Anticancer Res, 2019, 39(7):3767-3775
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.
S4353	Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S6435	Mequitazine Mequitazine is a histamine H1 antagonist which competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract.
S2078	Famotidine Famotidine (MK208) is a histamine H2–receptor antagonist with IC50 of 0.6 mM, commonly used to treat heartburn, GERD, ulcers, and other digestive conditions.	Anticancer Res, 2019, 39(7):3767-3775
S6469	Thonzylamine Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
S4293	Promethazine HCl Promethazine HCl is a potent histamine H₁ receptor antagonist, used as a sedative and antiallergic medication.	bioRxiv, 2020, 2020/9/20.4.7.30734 Anticancer Res, 2019, 39(7):3767-3775 Chem Biol Interact, 2019, 315:108888

Catalog No.	Information	Product Use Citations
S1357	Lidocaine Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.	Nat Biomed Eng, 2020, 4(3):286-297 J Cell Biochem, 2019, 120(10):16533-16542 Anticancer Res, 2019, 39(7):3767-3775
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.	Life Sci, 2019, 227:74-81
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.	Front Pharmacol, 2017, 8:667
S6612	Betazole Dihydrochloride Betazole Dihydrochloride is a histamine H2 agonist used clinically to test gastric secretory function.
S5498	Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S6569	VUF10460 VUF10460 is a histamine H4 receptor agonist.
S5619	Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S4382	Pyrilamine Maleate Pyrilamine Maleate (Mepyramine)is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling.

Choose Your Country or Region

By Signaling Pathways

By product type

Histamine Receptor

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Histamine Receptor Products