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Liver microsomal preparations are routinely used to predictdrug interactions that can occurin vivo as a result of inhi-bition of cytochrome P450 (CYP)-mediated metabolism.However, the concentration of free drug (substrate andinhibitor)at its intrahepatic site of action, a variable thatcannot be directly measured, may be significantly differentfrom that in microsomal incubation systems. Intact cellsmore closely reflect the environment to which CYP sub-strates and inhibitors are exposed in the liver, and it maytherefore be desirable to assess the potential of a drug tocause CYP inhibition in isolated hepatocytes....
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Báo cáo khoa học: Demethylation of radiolabelled dextromethorphan in rat microsomes and intact hepatocytes Kinetics and sensitivity to cytochrome P450 2D inhibitors
