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Histamine Receptor

Isoform-selective Products

H1 receptor H2 receptor H3 receptor H4 receptor

Signaling Pathway

Histamine Receptor Products

All (96)
Histamine Receptor Inhibitors (20)
Histamine Receptor Antagonists (67)
Histamine Receptor Agonists (9)
New Histamine Receptor Products

Catalog No.	Product Name	Information	Product Use Citations
S1847	Clemastine 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 Biomed Pharmacother, 2025, 185:117916 Nat Commun, 2024, 15(1):9837
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. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.	Front Cell Infect Microbiol, 2024, 14:1358873 Front Cell Infect Microbiol, 2024, 14:1358873 BMC Pharmacol Toxicol, 2024, 25(1):25
S1357	Lidocaine	Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.	Cell Rep, 2022, 38(10):110468 Exp Ther Med, 2021, 21(5):424 Nat Biomed Eng, 2020, 4(3):286-297
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.	Front Microbiol, 2022, 13:802409 J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5 Neuropharmacology, 2020, 168:108028
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
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
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 World J Gastroenterol, 2023, 29(20):3103-3118
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
S1291	Cetirizine DiHCl	Cetirizine DiHCl (Zyrtec, Reactine,UCB P071) is an antihistamine.	Viruses, 2024, 16(10)1559 Environ Toxicol Chem, 2021, 10.1002/etc.5018 J Allergy Clin Immunol, 2017, 139(4):1253-1265
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).	Environ Toxicol Chem, 2021, 10.1002/etc.5018 PLoS Pathog, 2020, 16;16(3):e1008341 Sci Rep, 2018, 8(1):15753
S2308	Hesperetin	Hesperetin is a bioflavonoid and, to be more specific, a flavanone.	J Transl Med, 2024, 22(1):208 Sci Rep, 2022, 12(1):7 Front Pharmacol, 2021, 12:735087
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
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
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
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
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
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 Front Cell Infect Microbiol, 2024, 14:1358873 Cell Rep Methods, 2023, 3(10):100599
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
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
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
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
S2585	Brompheniramine hydrogen maleate	Brompheniramine hydrogen maleate(Brompheniramine maleate) is a histamine H1 receptors antagonist.	Anticancer Res, 2019, 39(7):3767-3775
S2024	Ketotifen Fumarate	Ketotifen Fumarate(HC 20511 fumarate) is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer.	Environ Toxicol Chem, 2021, 10.1002/etc.5018
S3186	Azatadine dimaleate	Azatadine (SCH10649,Azatadine Maleate) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.	Pharmaceuticals (Basel), 2019, 12(4)
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
S4118	Histamine 2HCl	Histamine(Ceplene) is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.Histamine 2HCl can be used to induce animal models of Gastric and Intestinal Ulcers.	Front Pharmacol, 2017, 8:667
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
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. This product is a waxy solid.	Cancer Cell, 2025, 43(4):776-796.e14 Cancers (Basel), 2019, 11(12)
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
S4240	Doxylamine Succinate	Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.	Environ Toxicol Chem, 2021, 10.1002/etc.5018
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.	J Cell Commun Signal, 2023, 17(1):151-165
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.
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
S4253	Epinastine HCl	Epinastine (WAL-801CL) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.
S3146	Tripelennamine HCl	Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
S2494	Olopatadine HCl	Olopatadine HCl(ALO4943A,KW4679) 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.
E6012^New	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^New	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.
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. Histamine can be used to induce animal models of Gastric and Intestinal Ulcers.	Theranostics, 2024, 14(9):3719-3738 Life Sci, 2019, 227:74-81
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^New	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.
S4117	Histamine Phosphate	Histamine(Histamine diphosphate) acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors. Histamine Phosphate can be used to induce animal models of Gastric and Intestinal Ulcers.
S5864	Levocetirizine	Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.
E7255^New	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.
E4827^New	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
S4131	Levodropropizine	Levodropropizine((S)-(-)-Dropropizine,DF-526) 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.
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^New	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^New	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. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor.
S6612	Betazole Dihydrochloride	Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) is a histamine H2 agonist used clinically to test gastric secretory function.
S5196	Promethazine	Promethazine is a potent histamine H1 receptor antagonist. Promethazine is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. Promethazine exhibits antiparasitic properties.	Cancer Cell, 2025, 43(4):776-796.e14
S5498	Betahistine mesylate	Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S9459	Mecamylamine Hydrochloride	Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR(nicotinic acetylcholine receptors) antagonist.It is also a ganglionic blocker and can across the blood-brain barrier. It can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
S6569	VUF10460	VUF10460 is a histamine H4 receptor agonist.
E4873^New	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).
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(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.
E3778	Magnoliae Flos Extract	Magnoliae Flos Extract is isolated from Flos Magnoliae, which is an oriental medicinal herb commonly used for symptomatic relief from allergic rhinitis, sinusitis, and headache, by inhibiting histamine release from mast cells and cytokine secretion from T cells.
S3913	Pimethixene maleate	Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S4672	Dimenhydrinate	Dimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness.
S6835	3-deazaadenosine	3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM, and has anti-inflammatory, anti-proliferative and anti-HIV activity.
S5447	Triprolidine Hydrochloride	Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5619	Betahistine	Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
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 (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.
S0398	Astemizole	Astemizole (R 43512) 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.	Acta Pharm Sin B, 2023, 13(2):662-677 University of Valencia, 2023,
E6055^New	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.
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.
E4930^New	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.
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^New	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.
E4862^New	Pimethixene	Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT_2B 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.
S3176	Betahistine 2HCl	Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
S0897	Cyclizine	Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.
E4905^New	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.
S1291	Cetirizine DiHCl	Cetirizine DiHCl (Zyrtec, Reactine,UCB P071) is an antihistamine.	Viruses, 2024, 16(10)1559 Environ Toxicol Chem, 2021, 10.1002/etc.5018 J Allergy Clin Immunol, 2017, 139(4):1253-1265
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).	Environ Toxicol Chem, 2021, 10.1002/etc.5018 PLoS Pathog, 2020, 16;16(3):e1008341 Sci Rep, 2018, 8(1):15753
S2308	Hesperetin	Hesperetin is a bioflavonoid and, to be more specific, a flavanone.	J Transl Med, 2024, 22(1):208 Sci Rep, 2022, 12(1):7 Front Pharmacol, 2021, 12:735087
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
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
S2024	Ketotifen Fumarate	Ketotifen Fumarate(HC 20511 fumarate) is a fumaric acid salt of ketotifen which is a H1-antihistamine and mast cell stabilizer.	Environ Toxicol Chem, 2021, 10.1002/etc.5018
S3186	Azatadine dimaleate	Azatadine (SCH10649,Azatadine Maleate) is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.	Pharmaceuticals (Basel), 2019, 12(4)
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. This product is a waxy solid.	Cancer Cell, 2025, 43(4):776-796.e14 Cancers (Basel), 2019, 11(12)
S4240	Doxylamine Succinate	Doxylamine succinate competitively inhibits histamine at H1 receptors with substantial sedative and anticholinergic effects.	Environ Toxicol Chem, 2021, 10.1002/etc.5018
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(ALO4943A,KW4679) 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.
S4131	Levodropropizine	Levodropropizine((S)-(-)-Dropropizine,DF-526) 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.
S9459	Mecamylamine Hydrochloride	Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR(nicotinic acetylcholine receptors) antagonist.It is also a ganglionic blocker and can across the blood-brain barrier. It can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.
E3778	Magnoliae Flos Extract	Magnoliae Flos Extract is isolated from Flos Magnoliae, which is an oriental medicinal herb commonly used for symptomatic relief from allergic rhinitis, sinusitis, and headache, by inhibiting histamine release from mast cells and cytokine secretion from T cells.
S3913	Pimethixene maleate	Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S4672	Dimenhydrinate	Dimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness.
S6835	3-deazaadenosine	3-Deazaadenosine is an inhibitor of S-adenosylhomocysteine hydrolase, with a Ki of 3.9 µM, and has anti-inflammatory, anti-proliferative and anti-HIV activity.
S3176	Betahistine 2HCl	Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
S1847	Clemastine 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 Biomed Pharmacother, 2025, 185:117916 Nat Commun, 2024, 15(1):9837
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. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.	Front Cell Infect Microbiol, 2024, 14:1358873 Front Cell Infect Microbiol, 2024, 14:1358873 BMC Pharmacol Toxicol, 2024, 25(1):25
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.	Front Microbiol, 2022, 13:802409 J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5 Neuropharmacology, 2020, 168:108028
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
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
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 World J Gastroenterol, 2023, 29(20):3103-3118
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
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
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
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
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
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 Front Cell Infect Microbiol, 2024, 14:1358873 Cell Rep Methods, 2023, 3(10):100599
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
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
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
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
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
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
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.
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
S3146	Tripelennamine HCl	Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
E6012^New	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^New	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^New	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^New	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.
E4827^New	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
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^New	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^New	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. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor.
S5196	Promethazine	Promethazine is a potent histamine H1 receptor antagonist. Promethazine is a medication used in the management and treatment of allergic conditions, nausea and vomiting, motion sickness, and sedation. Promethazine exhibits antiparasitic properties.	Cancer Cell, 2025, 43(4):776-796.e14
E4873^New	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).
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(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.
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 (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.
S0398	Astemizole	Astemizole (R 43512) 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.	Acta Pharm Sin B, 2023, 13(2):662-677 University of Valencia, 2023,
E6055^New	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.
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.
E4930^New	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.
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^New	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.
E4862^New	Pimethixene	Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT_2B 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.
S0897	Cyclizine	Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.
E4905^New	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.
S1357	Lidocaine	Lidocaine (Alphacaine) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.	Cell Rep, 2022, 38(10):110468 Exp Ther Med, 2021, 21(5):424 Nat Biomed Eng, 2020, 4(3):286-297
S4118	Histamine 2HCl	Histamine(Ceplene) is an organic nitrogen compound, acts on target cells in mammalian brain via stimulation of Histamine 1/2.Histamine 2HCl can be used to induce animal models of Gastric and Intestinal Ulcers.	Front Pharmacol, 2017, 8:667
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.	J Cell Commun Signal, 2023, 17(1):151-165
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. Histamine can be used to induce animal models of Gastric and Intestinal Ulcers.	Theranostics, 2024, 14(9):3719-3738 Life Sci, 2019, 227:74-81
S4117	Histamine Phosphate	Histamine(Histamine diphosphate) acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors. Histamine Phosphate can be used to induce animal models of Gastric and Intestinal Ulcers.
S6612	Betazole Dihydrochloride	Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) 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.
E6012^New	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^New	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.
E4955^New	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.
E7255^New	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.
E4827^New	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
E7049^New	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.
E7890^New	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
E4873^New	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).
E6055^New	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.
E4930^New	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.
E4921^New	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.
E4862^New	Pimethixene	Pimethixene(Calmixen, Pimetixene) is a highly potent and non-selective antagonist of the 5-HT_2B 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.
E4905^New	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.

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