Histamine Receptor

Choose Selective Histamine Receptor Inhibitors

Histamine Receptor Signaling Pathway Map

Histamine Receptor Signaling Pathways

Histamine Receptor Products

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  • Histamine Receptor Inhibitors (17)
  • Histamine Receptor Antagonists (53)
  • Histamine Receptor Agonists (9)
  • New Histamine Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1291 Cetirizine DiHCl Cetirizine DiHCl (UCB P071) is an antihistamine.
Environ Toxicol Chem, 2021, 10.1002/etc.5018
J Allergy Clin Immunol, 2017, 139(4):1253-1265
J Allergy Clin Immunol, 2016, 10.1016/j.jaci.2016.03.028
S2024 Ketotifen Fumarate Ketotifen 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
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
Sci Rep, 2022, 12(1):7
Front Pharmacol, 2021, 12:735087
Carcinogenesis, 2020, 41(7):993-1004
S2494 Olopatadine HCl Olopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine.
S3052 Rupatadine Fumarate Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.
S3176 Betahistine 2HCl Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
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
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)
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
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.
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.
S4140 Buclizine HCl Buclizine HCl (UCB-4445) is an antihistamine and anticholinergic of the piperazine derivative family.
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.
S4672 Dimenhydrinate Dimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness.
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
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.
Cancers (Basel), 2019, 11(12)
E0164New 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.

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.
S0897 Cyclizine Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.
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 (SCH29851) 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.
EMBO Mol Med, 2021, e13929
Adv Ther (Weinh), 2020, 2000034
Cell Syst, 2019, 8(2):97-108
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
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
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
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
S1847 Clemastine (HS-592) fumarate Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
J Clin Invest, 2022, e152187
Neuroscience, 2022, S0306-4522(22)00001-X
Neuron, 2021, S0896-6273(21)00352-4
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
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.
S1890 Nizatidine Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
Anticancer Res, 2019, 39(7):3767-3775
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
Front Pharmacol, 2017, 8:693
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
S2065 Lafutidine Lafutidine (FRG-8813), a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
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.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
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.
S2552 Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Theranostics, 2021, 11(4):1828-1844
Int J Mol Sci, 2021, 22(16)9061
J Glob Antimicrob Resist, 2021, 27:167-171
S2585 Brompheniramine hydrogen maleate Brompheniramine hydrogen maleate is a histamine H1 receptors antagonist.
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
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.
J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5
Neuropharmacology, 2020, 168:108028
Mol Ther Methods Clin Dev, 2018, 11:83-91
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
J Cell Biochem, 2022, 10.1002/jcb.30213
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
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.
S3146 Tripelennamine HCl Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
S3721 Bilastine Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
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.
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
S4045 Pheniramine Maleate Pheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria.
S4139 Cyclizine 2HCl Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
S4262 Ebastine Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.
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
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.
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.
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
S5018 Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies.
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.
S5447 Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5479 Cloperastine hydrochloride Cloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
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.
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
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.
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).
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.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
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.
S5718 Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5864 Levocetirizine Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.
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.
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
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.
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.
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
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
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.
S5498 Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S5619 Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S6569 VUF10460 VUF10460 is a histamine H4 receptor agonist.
S6612 Betazole Dihydrochloride Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) is a histamine H2 agonist used clinically to test gastric secretory function.
S1291 Cetirizine DiHCl Cetirizine DiHCl (UCB P071) is an antihistamine.
Environ Toxicol Chem, 2021, 10.1002/etc.5018
J Allergy Clin Immunol, 2017, 139(4):1253-1265
J Allergy Clin Immunol, 2016, 10.1016/j.jaci.2016.03.028
S2024 Ketotifen Fumarate Ketotifen 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
S2308 Hesperetin Hesperetin is a bioflavonoid and, to be more specific, a flavanone.
Sci Rep, 2022, 12(1):7
Front Pharmacol, 2021, 12:735087
Carcinogenesis, 2020, 41(7):993-1004
S2494 Olopatadine HCl Olopatadine HCl is a histamine blocker and mast cell stabilizer with an IC50 of 559 μM for the release of histamine.
S3052 Rupatadine Fumarate Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 nM and 102 nM, respectively.
S3176 Betahistine 2HCl Betahistine (PT-9) is a histamine H3 receptor inhibitor with IC50 of 1.9 μM.
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
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)
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
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.
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.
S4140 Buclizine HCl Buclizine HCl (UCB-4445) is an antihistamine and anticholinergic of the piperazine derivative family.
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.
S4672 Dimenhydrinate Dimenhydrinate is an over-the-counter drug used to prevent nausea, vomiting, and dizziness caused by motion sickness.
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
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.
Cancers (Basel), 2019, 11(12)
E0164New 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.

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.
S0897 Cyclizine Cyclizine is a piperazine first-generation antagonist of histamine 1 receptor.
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 (SCH29851) 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.
EMBO Mol Med, 2021, e13929
Adv Ther (Weinh), 2020, 2000034
Cell Syst, 2019, 8(2):97-108
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
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
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
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
S1847 Clemastine (HS-592) fumarate Clemastine Fumarate (HS-592, Meclastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Clemastine stimulates autophagy via mTOR pathway.
J Clin Invest, 2022, e152187
Neuroscience, 2022, S0306-4522(22)00001-X
Neuron, 2021, S0896-6273(21)00352-4
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
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.
S1890 Nizatidine Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
Anticancer Res, 2019, 39(7):3767-3775
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
Front Pharmacol, 2017, 8:693
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
S2065 Lafutidine Lafutidine (FRG-8813), a newly developed histamine H(2)-receptor antagonist, inhibits gastric acid secretion.
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.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
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.
S2552 Azelastine HCl Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Theranostics, 2021, 11(4):1828-1844
Int J Mol Sci, 2021, 22(16)9061
J Glob Antimicrob Resist, 2021, 27:167-171
S2585 Brompheniramine hydrogen maleate Brompheniramine hydrogen maleate is a histamine H1 receptors antagonist.
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
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.
J Assoc Res Otolaryngol, 2021, 10.1007/s10162-021-00803-5
Neuropharmacology, 2020, 168:108028
Mol Ther Methods Clin Dev, 2018, 11:83-91
S3037 Bepotastine Besilate Bepotastine Besilate (TAU 284) is a non-sedating, selective antagonist of histamine 1 (H1) receptor with pIC50 of 5.7.
J Cell Biochem, 2022, 10.1002/jcb.30213
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00579-z
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.
S3146 Tripelennamine HCl Tripelennamine (Pyribenzamine) is a widely used H1 antagonist, inhibiting PhIP glucuronidation with IC50 of 30 μM.
S3721 Bilastine Bilastine is a new, well-tolerated, nonsedating H1 receptor antihistamine and has a rapid onset and prolonged duration of action.
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.
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
S4045 Pheniramine Maleate Pheniramine Maleate is an antihistamine with anticholinergic properties used to treat allergic conditions such as hay fever or urticaria.
S4139 Cyclizine 2HCl Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
S4262 Ebastine Ebastine is a potent H1-histamine receptor antagonist, used for allergic disorders.
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
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.
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.
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
S5018 Mebhydrolin napadisylate Mebhydrolin Napadisylate (Diazoline, Diazolin, Incidal, Omeril) is classified as an antihistamine drug classes used to treat allergies.
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.
S5447 Triprolidine Hydrochloride Triprolidine Hydrochloride is the hydrochloride salt form of Triprolidine, which is the first generation histamine H1 antagonist used in allergic rhinitis.
S5479 Cloperastine hydrochloride Cloperastine (HT-11) is a drug with a central antitussive effect, and is also endowed with an antihistaminic activity.
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.
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
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.
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).
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.
Calcif Tissue Int, 2021, 109(6):696-705
bioRxiv, 2021, 10.1101/2021.04.29.441931
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.
S5718 Acrivastine Acrivastine is an antihistamine medicine that relieves the symptoms of allergies.
S5864 Levocetirizine Levocetirizine (LCZ, (R)-Cetirizine), the R-enantiomer of cetirizine, is an antagonist of histamine H(1) receptor.
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.
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
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.
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.
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
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
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.
S5498 Betahistine mesylate Betahistine mesylate is the mesylate salt form of Betahistine, a histamine analog and H3 receptor agonist that serves as a vasodilator.
S5619 Betahistine Betahistine is an antivertigo drug that primarily acts as a histamine H1 agonist.
S6569 VUF10460 VUF10460 is a histamine H4 receptor agonist.
S6612 Betazole Dihydrochloride Betazole Dihydrochloride (Ametazole, 2-(3-Pyrazolyl)ethanamine) is a histamine H2 agonist used clinically to test gastric secretory function.
E0164New 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.