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Histamine Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
Verified customer review of Cetirizine DiHCl
S3208 Fexofenadine HCl Fexofenadine (MDL 16455A) inhibits histamine H1 receptor with IC50 of 246 nM.
Bone Res, 2025, 13(1):86
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)
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 Ki of 550 nM and 102 nM, respectively.
S4131 Levodropropizine Levodropropizine((S)-(-)-Dropropizine,DF-526) possess anti-allergic and inhibits histamine receptor, this compound reduces cough by interfering with stimulus activation of peripheral endings of sensory nerves and by modulation of neuropeptides involved in the cough reflex.
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.
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.
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
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. This compound 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. It 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
S5947 Amitriptyline Amitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. This compound is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. It 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)
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.
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.