Metabolism of 1'- and 4-hydroxymidazolam by glucuronide conjugation is largely mediated by UDP-glucuronosyltransferases 1A4, 2B4, and 2B7.

@article{Seo2010MetabolismO1,
  title={Metabolism of 1'- and 4-hydroxymidazolam by glucuronide conjugation is largely mediated by UDP-glucuronosyltransferases 1A4, 2B4, and 2B7.},
  author={Kyung-Ah Seo and Soo Hyeon Bae and Young Kil Choi and Chang Soo Choi and K Liu and Jae-Gook Shin},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2010},
  volume={38 11},
  pages={2007-13}
}
Midazolam undergoes oxidative hydroxylation by CYP3A to its metabolites, which are excreted mainly as glucuronidated conjugates into the urine. In this study, we examined the glucuronidation of hydroxymidazolam in human liver microsomes (HLMs) and characterized the UDP-glucuronosyltransferases (UGTs) involved in 1'- and 4-hydroxymidazolam glucuronidation. Among the 12 UGT isoforms tested, the O- and N-glucuronidation of 1'-hydroxymidazolam was mediated by UGT2B4/2B7 and 1A4, respectively. In… CONTINUE READING
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