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

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

生命薬学

研究成果: Contribution to journal › Article

39 被引用数 (Scopus)

抄録

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.

本文言語	英語
ページ（範囲）	395-401
ページ数	7
ジャーナル	Journal of Toxicological Sciences
巻	28
号	5
DOI	https://doi.org/10.2131/jts.28.395
出版ステータス	出版済み - 12 2003

All Science Journal Classification (ASJC) codes

Toxicology

文献へのアクセス

10.2131/jts.28.395

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引用スタイル

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AU - Yamada, Hideyuki

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AU - Nishio, Syunji

AU - Morioka, Takato

AU - Oguri, Kazuta

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AB - 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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