Histamine Receptor Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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
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 stabiliser 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) possesses anti-allergic properties 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 an 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 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.