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Histamine Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
S1847 Clemastine (HS-592) Fumarate Clemastine fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
Nat Commun, 2025, 16(1):1709
Nat Commun, 2025, 16(1):6382
Biomed Pharmacother, 2025, 185:117916
Verified customer review of Clemastine (HS-592) Fumarate
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
iScience, 2024, 27(10):110862
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S1358 Loratadine Loratadine is a histamine H1 receptor antagonist, used to treat allergies. This compound also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
Front Cell Infect Microbiol, 2024, 14:1358873
BMC Pharmacol Toxicol, 2024, 25(1):25
Cancer Cell, 2022, S1535-6108(22)00312-9
S2552 Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Biomed Pharmacother, 2024, 176:116766
UNIVERSITY OF PÉCS, 2023,
Front Pharmacol, 2022, 13:861295
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.
Front Microbiol, 2022, 13:802409
J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5
Neuropharmacology, 2020, 168:108028
S2044 Cyproheptadine HCl Cyproheptadine HCl(Periactin) is a hydrochloride salt form of cyproheptadine which is a histamine receptor antagonist.
Front Pharmacol, 2025, 16:1539032
World J Gastroenterol, 2023, 29(20):3103-3118
Cell Rep, 2020, 21;31(3):107548
S1845 Cimetidine Cimetidine (SKF-92334), a histamine congener, competitively inhibits histamine binding to histamine H2 receptors.
Cell Rep, 2021, 34(10):108832
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
S1890 Nizatidine Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
Gastroenterology, 2022, 162(4):1210-1225
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
S4262 Ebastine Ebastine(LAS-W 090,RP64305) is a potent H1-histamine receptor antagonist, used for allergic disorders.
Front Cell Infect Microbiol, 2024, 14:1358873
Cell Rep Methods, 2023, 3(10):100599
Zool Res, 2022, 43(3):457-468
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.
J Immunother Cancer, 2024, 12(11)e009805
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
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.
J Immunother Cancer, 2024, 12(11)e009805
Front Pharmacol, 2024, 15:1449178
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.
Biomolecules, 2025, 15(4)562
Anticancer Res, 2019, 39(7):3767-3775
Nature, 2018, 560(7718):372-376
Verified customer review of Hydroxyzine 2HCl
S5662 Ranitidine Ranitidine(AH-19065) is an H2 histamine receptor antagonist that works by blocking histamine and thus decreasing the amount of acid released by cells of the stomach.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
Anticancer Res, 2019, 39(7):3767-3775
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
Chem Biol Interact, 2019, 315:108888
Anticancer Res, 2019, 39(7):3767-3775
S1382 Mianserin HCl Mianserin (Bolvidon, Norval, Tolvon,ORG GB-94 HCl,Mianserin hydrochloride) is an potent antagonist of H1 histamine receptor and 5-HT serotonin receptors, used for the treatment of depression.
Alzheimers Dement, 2023, 10.1002/alz.13090
Immunity, 2019, 50(5):1163-1171
S1801 Ranitidine Hydrochloride Ranitidine (AH19065) is a histamine H2-receptor antagonist, used to treat stomach or intestinal ulcers.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
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,Meclozine dihydrochloride) 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
Front Pharmacol, 2017, 8:693
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
S0398 Astemizole Astemizole (R 43512) is a histamine H1-receptor antagonist with IC50 of 4.7 nM. This compound is also a potent inhibitor of ether à-go-go 1 (Eag1) and Eag-related gene (Erg) potassium channels. It has antineoplastic and antipruritic effects.
Acta Pharm Sin B, 2023, 13(2):662-677
University of Valencia, 2023,
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
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.
Toxicol Lett, 2025, 406:31-37
S2065 Lafutidine Lafutidine (FRG-8813), a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
Front Immunol, 2024, 15:1417398
S2585 Brompheniramine hydrogen maleate Brompheniramine hydrogen maleate(Brompheniramine maleate) is a histamine H1 receptors antagonist.
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
E4827 Diphenhydramine Diphenhydramine is a first-generation antihistamine and sedative that acts as an antagonist of the H1 receptor and is used for treating acute allergic reactions. It is FDA-approved as an adjunct to epinephrine and corticosteroids and exhibits anticholinergic and antiemetic effects.
Int J Mol Sci, 2024, 25(18)10162
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.
J Cell Biochem, 2022, 10.1002/jcb.30213
S5196 Promethazine Promethazine is a potent histamine H1 receptor antagonist. This compound is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. It exhibits antiparasitic properties.
Cancer Cell, 2025, 43(4):776-796.e14
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
S3146 Tripelennamine HCl Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
E6012 Cetirizine Cetirizine is a second-generation, non-sedating selective antagonist of H1 histamine receptors. It has anti-inflammatory and anti-allergic properties and is used to treat perennial rhinitis and urticaria.
E4938 Diphenylpyraline Diphenylpyraline(Allergen, Difenilpiralina; 4-Diphenylmethoxy-1-methylpiperidine), also known as 4-Diphenylmethoxy-1-methylpiperidine, is a first-generation antihistamine that acts as an antagonist of the histamine H1 receptor. It provides therapeutic antiallergic effects and has the potential to treat cocaine addiction.
E1796 Dimethindene maleate Dimethindene maleate is a selective antagonist of histamine H1 and exhibits antihistamine effects. It suppresses the cromakalim-induced/glibenclamide-sensitive K+ currents in a concentration-dependent and reversible manner.
E4955 Pitolisant Pitolisant(BF2.649, Tiprolisant) is a potent, selective antagonist of the non-imidazole histamine H3 receptor, with a Ki value of 0.16 nM and an EC50 of 1.5 nM as an inverse agonist. It enhances the activity of histaminergic neurons, promoting vigilance and cognitive function. It is useful in research on wakefulness, memory deficits, and cognitive disorders.
S5864 Levocetirizine Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.
E7255 Rupatadine Rupatadine (UR-12592) is a potent, orally active and long-lasting dual antagonist of platelet-activating factor (PAF) and histamine (H1) with Ki of 0.55 μM and 0.1 μM, respectively. It exhibits anti-fibrosis effect and can be used in research on treatments for pulmonary fibrosis, allergic and inflammatory conditions involving both platelet-activating factor (PAF) and histamine.
E0164 Antazoline Phosphate

Antazoline Phosphate is the phosphate salt of antazoline. Antazoline is a first-generation antihistaminic agent and acts as a histamine H1 receptor antagonist.
E7049 Fexofenadine Fexofenadine (MDL-16455, Terfenadine carboxylate) is a non anticholinergic and non sedative second-generation antagonist of histamine (H1) receptor. It can be used in research to treat allergic disorders by suppressing eosinophilia and systemic anaphylaxis, especially in allergic rhinitis and chronic urticaria.
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.
E7890 Ketotifen Ketotifen is an antagonist of the histamine 1 (H1) receptor and a mast cell stabilising agent that decreases visceral hypersensitivity and improves intestinal symptoms in patients with irritable bowel syndrome. It also inhibits SARS-CoV-2 with an EC50 of 48.9 μM
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. This compound 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.
S1880 Roxatidine Acetate HCl Roxatidine Acetate HCl(HOE 760) 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(BW825C) is an antihistamine medicine that relieves the symptoms of allergies.
E7924New GSK189254A GSK189254A (GSK189254 free base) is a histamine H3 receptor antagonist with pKi values of 9.59-9.90 for human H3 and 8.51-9.17 for rat H3.
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.
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 (Tiprolisant, BF-2649) 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.
E6055New Epinastine Epinastine (WAL801) is potent nonsedative antiallergic agent and an antagonist of histamine H1 receptor. It inhibits the actions of leukotrienes, platelet-activating factor (PAF), and bradykinin. It also stabilizes mast cells and reduces IL-8 release from eosinophils, helping to control allergic inflammation.
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.
S6435 Mequitazine Mequitazine (LM-209) 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.
S6469 Thonzylamine Thonzylamine (Neohetramine) is an antihistamine and anticholinergic drug.
E4921 Azelastine Azelastine(Azelastina; Astelin) is a potent antihistaminic and antiallergic drug, an antagonist of the histamine H1 receptor. It is also effective in treating allergic rhinitis, bronchial asthma, and SARS-CoV-2 and has shown potential in ameliorating aortic calcification, increasing apoA expression, and reducing apoB levels.
S0897 Cyclizine Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.
E4905 Cyclizine hydrochloride Cyclizine hydrochloride is an antagonist of the H1 histamine receptor used for the treatment and prevention of vertigo and motion sickness. It also exhibits antihistaminic properties.
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.
E4873 Mebhydroline Mebhydroline acts as a selective antagonist of farnesoid X receptor (FXR). Mebhydrolin improves blood glucose balance in in vivo mice models by inhibiting hepatic gluconeogenesis through the FXR/miR-22-3p/PI3K/AKT/FoxO1 pathway and enhancing glycogen synthesis. It also acts as a specific antagonist of histamine H1 receptor. It has potential for its use in the treatment of Type 2 diabetes mellitus (T2DM).
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.
S5018 Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies.
S4353 Terfenadine Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. This compound is a potent open-channel blocker of hERG with an IC50 of 204 nM. This chemical, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. It induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
E4930 Asenapine Asenapine(Org 5222, HSDB8061) is a multi-target receptor antagonist. It acts as an antagonist of serotonin receptors with pKi values of 8.4-10.5, adrenoceptors with pKi values of 8.9-9.5, dopamine receptors with pKi values of 8.9-9.4 and histamine receptors with pKi values of 8.2-9.0.
E4862 Pimethixene Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT2B receptor, with a pKi of 10.44. It also functions as an antihistamine and anticholinergic agent, and is a highly potent multi-target antagonist with antagonistic effects on multiple receptors.