Identification of human cytochrome P450 enzymes involved in the formation of 4-hydroxyestazolam from estazolam

@article{Miura2005IdentificationOH,
  title={Identification of human cytochrome P450 enzymes involved in the formation of 4-hydroxyestazolam from estazolam},
  author={Masatomo Miura and Koichi Otani and Tadashi Ohkubo},
  journal={Xenobiotica},
  year={2005},
  volume={35},
  pages={455 - 465}
}
To predict drug interactions with estazolam, the biotransformation of estazolam to its major hydoxylated metabolite, 4-hydroxyestazolam was studied in vitro using pooled human liver microsomes and individual expressed human cytochrome P450 (CYP) enzymes. Estazolam was metabolized to 4-hydroxyestazolam according to the Hill kinetic model in pooled human liver microsomes. The Km value for the 4-hydroxylation of estazolam was 24.1 µM, and the Vmax value was 52.6 pmol min−1 mg−1 protein. The… 
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