VERAPAMIL IMPURITY J
VERAPAMIL IMPURITY J 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 |
| 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 用途与合成方法
Calcium channel blocker
P-glycoprotein (P-gp) inhibitor
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.
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. |
