Desethylchloroquine-d4 is intended for use as an internal standard for the quantification of desethylchloroquine by GC- or LC-MS. Desethylchloroquine is a major active metabolite of chloroquine .1 Desethylchloroquine is formed when chloroquine undergoes dealkylation, primarily by the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 and to a lesser extent by CYP2D6. It inhibits the growth of the P. falciparum strain LA136 in vitro (IC50 = 9.9 ng/ml).2
1.Projean, D., Baune, B., Farinotti, R., et al.In vitro metabolism of chloroquine: Identification of CYP2C8, CYP3A4, and CYP2D6 as the main isoforms catalyzing N-desethylchloroquine formationDrug Metab. Dispos.31(6)748-754(2003) 2.Aderounmu, F.A.In vitro assessment of the antimalarial activity of chloroquine and its major metabolitesAnn. Trop. Med. Parasitol.78(6)581-585(1984)