Formation of highly analgesic morphine-6-glucuronide following physiologic concentration of morphine in human brain

Hideyuki Yamada, Kumiko Ishii, Yuji Ishii, Ichiro Ieiri, Syunji Nishio, Takato Morioka, Kazuta Oguri

Research output: Contribution to journalArticle

39 Citations (Scopus)

Abstract

3H-Morphine at physiologic concentration was metabolized in vitro to its 3- and 6-glucuronides by human brain homogenate. Recombinant UGT2B7, one of the UDP-glucuronosyltransferase (UGT) isoforms, is able to glucuronidate the 3- and 6-hydroxy groups of morphine at nanomolar concentrations. These results suggest that endogenous morphine is converted to its 6-glucuronide, a more highly analgesic substance than the parent compound, to suppress effectively pain symptoms in humans.

Original languageEnglish
Pages (from-to)395-401
Number of pages7
JournalJournal of Toxicological Sciences
Volume28
Issue number5
DOIs
Publication statusPublished - Dec 2003

All Science Journal Classification (ASJC) codes

  • Toxicology

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