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67018-85-3

中文名称 VERAPAMIL IMPURITY J
英文名称 NORVERAPAMIL
CAS 67018-85-3
分子式 C26H36N2O4
分子量 440.58
MOL 文件 67018-85-3.mol
更新日期 2023/09/05 14:18:02
67018-85-3 结构式 67018-85-3 结构式

基本信息

中文别名
维拉帕米EP杂质J
化合物 T12244
盐酸维拉帕米杂质J(EP) 标准品
英文别名
D591
NORVERAPAMIL
Norverapamil D6
Verapamil Impurity J
Verapamil EP Impurity J Monomer
(2RS)-2-(3,4-Dimethoxy-phenyl)-5-[[
2-(3,4-Dimethoxyphenyl)-2-isopropyl-5-(3,4-dimethoxyphenethylamino)valeronitrile
5-[(3,4-dimethoxyphenethyl)amino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile
α-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-isopropylbenzeneacetonitrile
Benzeneacetonitrile, α-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-(1-methylethyl)-

物理化学性质

沸点586.1±50.0 °C(Predicted)
密度1.063±0.06 g/cm3(Predicted)
酸度系数(pKa)9.79±0.19(Predicted)
CAS 数据库67018-85-3

安全数据

危险性符号(GHS)
GHS06
警示词危险
危险性描述H301

常见问题列表

生物活性
Norverapamil ((±)-Norverapamil),是 Verapamil 的 N-去甲基代谢物,是一种钙通道 (L-type calcium channel) 阻滞剂和 P-糖蛋白 (P-gp) 功能抑制剂。
靶点

Calcium channel blocker
P-glycoprotein (P-gp) inhibitor

体外研究

Norverapamil ((±)-Norverapamil) is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs. norverapamil, also inhibits macrophage-induced tolerance and achieves similar serum levels to verapamil.
Verapamil and its major metabolite Norverapamil were identified to be both mechanism-based inhibitors and substrates of CYP3A and reported to have non-linear pharmacokinetics in clinic.

体内研究

Norverapamil (9 mg/kg; p.o.), a major metabolite of verapamil, has terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng▪h/ml, and 41.6 ng/mL, respectively.

Animal Model: Male Sprague-Dawley rats
Dosage: 9 mg/kg (Pharmacokinetic Study)
Administration: Oral administration
Result: t 1/2 =9.4 hours; AUC=260 ng▪h/mL; C max =41.6 ng/mL.
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