| Bioactivity | Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor[1][2]. |
| Target | Calcium channel blockerP-glycoprotein (P-gp) inhibitor |
| Invitro | 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[1]. 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[3]. |
| 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[4]. Animal Model: |
| Name | Norverapamil |
| CAS | 67018-85-3 |
| Formula | C26H36N2O4 |
| Molar Mass | 440.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Adams KN, et al. Verapamil, and its metabolite norverapamil, inhibit macrophage-induced, bacterial efflux pump-mediated tolerance to multiple anti-tubercular drugs. J Infect Dis. 2014 Aug 1;210(3):456-66. [2]. Pauli-Magnus C, et al. Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein. J Pharmacol Exp Ther. 2000 May;293(2):376-82. [3]. Wang J et al. A semi-physiologically-based pharmacokinetic model characterizing mechanism-based auto-inhibition to predict stereoselective pharmacokinetics of verapamil and its metabolite norverapamil in human. Eur J Pharm Sci. 2013 Nov 20;50(3-4):290-302 [4]. Choi DH, et al. Effects of simvastatin on the pharmacokinetics of verapamil and its main metabolite, norverapamil, in rats. Eur J Drug Metab Pharmacokinet. 2009 Jul-Sep;34(3-4):163-8. |
Norverapamil
CAS: 67018-85-3 F: C26H36N2O4 W: 440.58
Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P
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