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编 号：F421704
分子式：C26H36N2O4
分子量：440.58
分子式：C26H36N2O4
分子量：440.58
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CAS No: 67018-85-3
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生物活性：
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
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:t1/2=9.4 hours;AUC=260 ng?h/mL;Cmax=41.6 ng/mL.
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.
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
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:t1/2=9.4 hours;AUC=260 ng?h/mL;Cmax=41.6 ng/mL.
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.
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