Literature DB >> 14746343

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

Hideyuki Yamada1, Kumiko Ishii, Yuji Ishii, Ichiro Ieiri, Syunji Nishio, Takato Morioka, Kazuta Oguri.   

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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Year:  2003        PMID： 14746343     DOI： 10.2131/jts.28.395

Source DB:  PubMed          Journal:  J Toxicol Sci        ISSN： 0388-1350            Impact factor:   2.196


  9 in total

Review 1.  Role of morphine's metabolites in analgesia: concepts and controversies.

Authors:  Erica Wittwer; Steven E Kern
Journal:  AAPS J       Date:  2006-05-26       Impact factor: 4.009

2.  Computational framework for predictive PBPK-PD-Tox simulations of opioids and antidotes.

Authors:  Carrie German; Minu Pilvankar; Andrzej Przekwas
Journal:  J Pharmacokinet Pharmacodyn       Date:  2019-08-08       Impact factor: 2.745

3.  Nicotine regulates the expression of UDP-glucuronosyltransferase (UGT) in humanized UGT1 mouse brain.

Authors:  Masaya Sakamoto; Tomoo Itoh; Robert H Tukey; Ryoichi Fujiwara
Journal:  Drug Metab Pharmacokinet       Date:  2015-05-07       Impact factor: 3.614

Review 4.  Pharmacology of morphine in obese patients: clinical implications.

Authors:  Célia Lloret Linares; Xavier Declèves; Jean Michel Oppert; Arnaud Basdevant; Karine Clement; Christophe Bardin; Jean Michel Scherrmann; Jean Pierre Lepine; Jean François Bergmann; Stéphane Mouly
Journal:  Clin Pharmacokinet       Date:  2009       Impact factor: 6.447

Review 5.  Morphine metabolism, transport and brain disposition.

Authors:  Simona De Gregori; Manuela De Gregori; Guglielmina Nadia Ranzani; Massimo Allegri; Cristina Minella; Mario Regazzi
Journal:  Metab Brain Dis       Date:  2011-12-24       Impact factor: 3.584

Review 6.  The opioid epidemic: a central role for the blood brain barrier in opioid analgesia and abuse.

Authors:  Charles P Schaefer; Margaret E Tome; Thomas P Davis
Journal:  Fluids Barriers CNS       Date:  2017-11-29

Review 7.  Alterations of Cytochrome P450s and UDP-Glucuronosyltransferases in Brain Under Diseases and Their Clinical Significances.

Authors:  Yun Sheng; Hanyu Yang; Tong Wu; Liang Zhu; Li Liu; Xiaodong Liu
Journal:  Front Pharmacol       Date:  2021-04-21       Impact factor: 5.810

8.  An inverse association between plasma benzoxazinoid metabolites and PSA after rye intake in men with prostate cancer revealed with a new method.

Authors:  Elise Nordin; Stine K Steffensen; Bente B Laursen; Sven-Olof Andersson; Jan-Erik Johansson; Per Åman; Göran Hallmans; Michael Borre; Dan Stærk; Kati Hanhineva; Inge S Fomsgaard; Rikard Landberg
Journal:  Sci Rep       Date:  2022-03-28       Impact factor: 4.379

9.  Endogenous morphine in SH-SY5Y cells and the mouse cerebellum.

Authors:  Arnaud Muller; Elise Glattard; Omar Taleb; Véronique Kemmel; Alexis Laux; Monique Miehe; François Delalande; Guy Roussel; Alain Van Dorsselaer; Marie-Hélène Metz-Boutigue; Dominique Aunis; Yannick Goumon
Journal:  PLoS One       Date:  2008-02-20       Impact factor: 3.240
  9 in total

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