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Norverapamil

CAS No. : 67018-85-3

MCE 站：Norverapamil

产品活性：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。

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 ((±)-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.

In Vivo: 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.

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