| Identification | Back Directory | [Name]
NORVERAPAMIL | [CAS]
67018-85-3 | [Synonyms]
D591
NORVERAPAMIL
Norverapamil D6
Verapamil Impurity J
2-(3,4-Dimethoxyphenyl)-2-isopropyl-5-(3,4-dimethoxyphenethylamino)valeronitrile
5-[(3,4-dimethoxyphenethyl)amino]-2-(3,4-dimethoxyphenyl)-2-isopropylvaleronitrile
α-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]amino]propyl]-3,4-dimethoxy-α-isopropylbenzeneacetonitrile
Benzeneacetonitrile, a-[3-[[2-(3,4-dimethoxyphenyl)-ethyl]amino]propyl]-3,4-dimethoxy-a-(1-methylethyl)- | [EINECS(EC#)]
266-544-8 | [Molecular Formula]
C26H36N2O4 | [MDL Number]
MFCD00871831 | [MOL File]
67018-85-3.mol | [Molecular Weight]
440.58 |
| Hazard Information | Back Directory | [Chemical Properties]
Yellowish to brownish oil | [Uses]
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]. | [Definition]
ChEBI:2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl]amino}-2-(propan-2-yl)pentanenitrile is a secondary amino compound that is 3,4-dimethoxyphenylethylamine in which one of the hydrogens attached to the nitrogen has been replaced by a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group. It is an aromatic ether, a nitrile, a polyether and a secondary amino compound. | [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: | Male Sprague-Dawley rats[4] | | 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.
|
| [IC 50]
L-type calcium channel | [References]
[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. DOI:10.1093/infdis/jiu095
[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. PMID:10773005
[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. DOI:10.1016/j.ejps.2013.07.012
[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. DOI:10.1007/BF03191168 |
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