The Journal of Toxicological Sciences
Online ISSN : 1880-3989
Print ISSN : 0388-1350
ISSN-L : 0388-1350
Regular Paper
FORMATION OF HIGHLY ANALGESIC MORPHINE-6-GLUCURONIDE FOLLOWING PHYSIOLOGIC CONCENTRATION OF MORPHINE IN HUMAN BRAIN
Hideyuki YAMADAKumiko ISHIIYuji ISHIIIchiro IEIRISyunji NISHIOTakato MORIOKAKazuta OGURI
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2003 Volume 28 Issue 5 Pages 395-401

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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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© 2003 The Japanese Society of Toxicology
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