VERAPAMIL IMPURITY J
- CAS号:67018-85-3
- 英文名:NORVERAPAMIL
- 中文名:VERAPAMIL IMPURITY J
- CBNumber:CB0223348
- 分子式:C26H36N2O4
- 分子量:440.58
- MOL File:67018-85-3.mol
- 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
- EPA化学物质信息 :Benzeneacetonitrile, .alpha.-[3-[[2-(3,4-dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-.alpha.-(1-methylethyl)- (67018-85-3)
VERAPAMIL IMPURITY J性质、用途与生产工艺
- 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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