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J Toxicol Sci. 2003 Dec;28(5):395-401.

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

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Laboratory of Molecular Life Science, Graduate School of Pharmaceutical Sciences, Kyushu University, 3-1-1 Maidashi, Higashi-ku, Fukuoka 812-8582, Japan.


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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