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CAS No. : 67812-42-4
MCE 国际站:Norverapamil hydrochloride
产品活性:Norverapamil hydrochloride,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。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling | Metabolic Enzyme/Protease
作用靶点:Calcium Channel | P-glycoprotein | Drug Metabolite
In Vitro: 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. 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.
In Vivo: Norverapamil hydrochloride (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.
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