Enzyme kinetic parameters for midazolam were time-dependent in human liver microsomes, under initial velocity conditions. Vmax and Km decreased up to 3.7 and 3.1-fold, respectively, for 10 min compared to 1 min incubations. Mathematical models describing the relationship between inactivation and the time-dependency of enzyme kinetic parameter estimates were derived and discussed.
Keywords: Enzyme kinetics, midazolam, mechanism based inactivation, time-dependent inactivation
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