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

doi:10.2131/jts.28.395

Regular Paper

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

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Keywords: Endogenous morphine, Morphine-6-glucuronide, UDP-glucuronosyltransferase, Human brain

JOURNAL FREE ACCESS

2003 Volume 28 Issue 5 Pages 395-401

DOI https://doi.org/10.2131/jts.28.395

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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.

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