Norverapamil hydrochloride是 Verapamil 的 N-去甲基代谢物，是L型钙通道阻滞剂和 P-糖蛋白 (P-gp) 功能抑制剂。

Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) is an N-demethylated metabolite of Verapamil and it is an L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.

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 the clinic. Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) is similarly effective as verapamil at inhibiting isoniazid and rifampicin tolerance and killing of intracellular M. tuberculosis in the absence of other drugs [1][3].

Norverapamil hydrochloride (9 mg/kg; p.o.) has a terminal half-life, AUC and Cmax values of 9.4 hours, 260 ng?h/ml, and 41.6 ng/mL, respectively[4].

67812-42-4

C26H37ClN2O4

477.04

(±)-Norverapamil hydrochloride;D591 hydrochloride;盐酸去甲维拉帕米

H2O:50 mg/mL (104.81 mM)
DMSO:31 mg/mL (64.98 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years