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

KA Seo, SK Bae, YK Choi, CS Choi, KH Liu…

Index: Seo, Kyung-Ah; Bae, Soo Kyung; Choi, Young-Kil; Choi, Chang Soo; Liu, Kwang-Hyeon; Shin, Jae-Gook Drug Metabolism and Disposition, 2010 , vol. 38, # 11 p. 2007 - 2013

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Citation Number: 29

Abstract

Abstract 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- ...