Biphasic Kinetics of Imipramine N-Oxidation in Rat Brain Microsomes

概要

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Imipramine (IMI) N-oxidase activity in brain microsomes from rats of both sexes was determined by high performance liquid chromatography, and compared with the results in rat liver microsomes. Brain and liver microsomal IMI N-oxidation was sensitive to thermal inactivation and had an optimal pH at around 9.0. IMI N-oxidase activity (15.54 pmol/mim/mg protein) in brain microsomes was about one-hundredth that of liver microsomes (2.08 nmol/min/mg protein) at a substrate concentration of 5 mM. IMI N-oxidase activities in both brain and liver microsomes displayed biphasic kinetics that associated a low K_m-low V_<max> element with a high K_m-high V_<max> component. Furthermore, a significant sex difference was observed in V_<max> values (male>female) in both phases, but K_m values were similar between male and female rats, resulting in a sigmificant sex difference (male>female) in intrinsic clearance values (V_<max>/K_m) of the low-K_m and the high-K_m phases.
公益社団法人日本薬学会の論文
1999-03-15