产品说明书

Chlorpheniramine maleate

Print
Chemical Structure| 113-92-8 同义名 : Chlorphenamine maleate;Chlorpheniramine (maleate);Chlor-100;Chlo-Amine;Bayer Brand of Chlorpheniramine Maleate;Neorestamin;Deconamine;Chlortrimeton;Piriton;Chlorprophenpyridamine;(±)-Chlorpheniramine;NCI-C55265
CAS号 : 113-92-8
货号 : A352417
分子式 : C20H23ClN2O4
纯度 : 99%
分子量 : 390.86
MDL号 : MFCD00069225
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(268.64 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 30 mg/mL(76.75 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • H1 receptor

    Histamine H1 receptor, IC50:12 nM
描述 Chlorpheniramine Maleate is potent, less sedative antihistaminic drug, which acts by inhibiting histamine release from mast cells. Chlorpheniramine causes bronchodilation during resting period by acting on the circulating or tissue histamine in asthmatics which contributes to an increase in resting bronchomotor tone[3]. Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds. Age, dialysis, urinary pH and flow influence the elimination kinetics of chlorpheniramine[4]. A nasal gel formulation for an antihistaminic drug, Chlorpheniramine maleate (CPM), which suffers from poor oral[5]. The antihistamine chlorpheniramine maleate (CPM) is also used for symptomatic relief of hypersensitive reactions and in pruritic skin disorders[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.56mL

0.51mL

0.26mL

12.79mL

2.56mL

1.28mL

25.58mL

5.12mL

2.56mL
参考文献

[1]Medina MA, Garcia de Veas R, et al. Chlorpheniramine inhibits the synthesis of ornithine decarboxylase and the proliferation of human breast cancer cell lines. Breast Cancer Res Treat. 1995 Aug;35(2):187-94.

[2]Sleevi MC, Cale AD Jr, et al. Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines. J Med Chem. 1991 Apr;34(4):1314-28.

[3]Chugh J, Yadav YR, Kulkarni HS, Maheshwari S. The Effect of Aerosolized Chlorpheniramine Maleate on Exercise Induced Bronchospasm and Gas Exchange in Asthmatics. J Assoc Physicians India. 2020 Apr;68(4):21-25

[4]Rumore MM. Clinical pharmacokinetics of chlorpheniramine. Drug Intell Clin Pharm. 1984 Sep;18(9):701-7

[5]Soliman II, Soliman NA, Abdou EM. Formulation and stability study of chlorpheniramine maleate nasal gel. Pharm Dev Technol. 2010 Sep-Oct;15(5):484-91

[6]Ceschel GC, Maffei P, Gentile M. Design and evaluation of a new transdermal formulation containing chlorpheniramine maleate. Drug Dev Ind Pharm. 1999 Sep;25(9):1035-9