Kinetic Characterization and Identification of the Enzymes Responsible for the Hepatic Biotransformation of Adinazolam and N??Desmethyladinazolam in Man

K Venkatakrishnan, LL Moltke, SX Duan…

Index: Venkatakrishnan, Karthik; Von Moltke, Lisa L.; Duan, Su Xiang; Fleishaker, Joseph C.; Shader, Richard I.; Greenblatt, David J. Journal of Pharmacy and Pharmacology, 1998 , vol. 50, # 3 p. 265 - 274

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Citation Number: 41

Abstract

Abstract The kinetics of the N-demethylation of adinazolam to N-desmethyladinazolam (NDMAD), and of NDMAD to didesmethyladinazolam (DDMAD), were studied with human liver microsomes using substrate concentrations in the range 10–1000 μ m. The specific cytochrome P450 (CYP) isoforms mediating the biotransformations were identified using microsomes containing specific recombinant CYP isozymes expressed in human lympho- ...