Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor.

@article{Lu2003MechanismbasedIO,
  title={Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor.},
  author={Ping Lu and Michael L. Schrag and Donald E. Slaughter and Conrad E. Raab and Magang Shou and A. David Rodrigues},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2003},
  volume={31 11},
  pages={
          1352-60
        }
}
  • P. LuM. Schrag A. D. Rodrigues
  • Published 1 November 2003
  • Biology, Chemistry
  • Drug metabolism and disposition: the biological fate of chemicals
Zileuton, a 5-lipoxygenase inhibitor, was evaluated as an inhibitor of cytochrome P450 activity in human liver microsomes. In the absence of preincubation, the racemate was found to be a weak inhibitor (IC50 > 100 microM) of phenacetin O-deethylation (POD) (CYP1A2), paclitaxel 6alpha-hydroxylation (CYP2C8), diclofenac 4'-hydroxylation (CYP2C9), (S)-mephenytoin 4'-hydroxylation (CYP2C19), bufuralol 1'-hydroxylation (CYP2D6), testosterone 6beta-hydroxylation (CYP3A4), chlorzoxazone 6… 

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