Morphine metabolism, transport and brain disposition

The chemical structures of morphine and its metabolites are closely related to the clinical effects of drugs (analgesia and side-effects) and to their capability to cross the Blood Brain Barrier (BBB). Morphine-6-glucuronide (M6G) and Morphine-3-glucuronide (M3G) are both highly hydrophilic, but onl...

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Detalles Bibliográficos
Autores principales: De Gregori, Simona, De Gregori, Manuela, Ranzani, Guglielmina Nadia, Allegri, Massimo, Minella, Cristina, Regazzi, Mario
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer US 2011
Materias:
Review Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3276770/
https://www.ncbi.nlm.nih.gov/pubmed/22193538
http://dx.doi.org/10.1007/s11011-011-9274-6
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author De Gregori, Simona
De Gregori, Manuela
Ranzani, Guglielmina Nadia
Allegri, Massimo
Minella, Cristina
Regazzi, Mario
author_facet De Gregori, Simona
De Gregori, Manuela
Ranzani, Guglielmina Nadia
Allegri, Massimo
Minella, Cristina
Regazzi, Mario
author_sort De Gregori, Simona
collection PubMed
description The chemical structures of morphine and its metabolites are closely related to the clinical effects of drugs (analgesia and side-effects) and to their capability to cross the Blood Brain Barrier (BBB). Morphine-6-glucuronide (M6G) and Morphine-3-glucuronide (M3G) are both highly hydrophilic, but only M6G can penetrate the BBB; accordingly, M6G is considered a more attractive analgesic than the parent drug and the M3G. Several hypotheses have been made to explain these differences. In this review we will discuss recent advances in the field, considering brain disposition of M6G, UDP-glucoronosyltransferases (UGT) involved in morphine metabolism, UGT interindividual variability and transport proteins.
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spelling pubmed-32767702012-03-01 Morphine metabolism, transport and brain disposition De Gregori, Simona De Gregori, Manuela Ranzani, Guglielmina Nadia Allegri, Massimo Minella, Cristina Regazzi, Mario Metab Brain Dis Review Article The chemical structures of morphine and its metabolites are closely related to the clinical effects of drugs (analgesia and side-effects) and to their capability to cross the Blood Brain Barrier (BBB). Morphine-6-glucuronide (M6G) and Morphine-3-glucuronide (M3G) are both highly hydrophilic, but only M6G can penetrate the BBB; accordingly, M6G is considered a more attractive analgesic than the parent drug and the M3G. Several hypotheses have been made to explain these differences. In this review we will discuss recent advances in the field, considering brain disposition of M6G, UDP-glucoronosyltransferases (UGT) involved in morphine metabolism, UGT interindividual variability and transport proteins. Springer US 2011-12-24 2012 /pmc/articles/PMC3276770/ /pubmed/22193538 http://dx.doi.org/10.1007/s11011-011-9274-6 Text en © The Author(s) 2011 https://creativecommons.org/licenses/by-nc/4.0/ This article is distributed under the terms of the Creative Commons Attribution Noncommercial License which permits any noncommercial use, distribution, and reproduction in any medium, provided the original author(s) and source are credited.
spellingShingle Review Article
De Gregori, Simona
De Gregori, Manuela
Ranzani, Guglielmina Nadia
Allegri, Massimo
Minella, Cristina
Regazzi, Mario
Morphine metabolism, transport and brain disposition
title Morphine metabolism, transport and brain disposition
title_full Morphine metabolism, transport and brain disposition
title_fullStr Morphine metabolism, transport and brain disposition
title_full_unstemmed Morphine metabolism, transport and brain disposition
title_short Morphine metabolism, transport and brain disposition
title_sort morphine metabolism, transport and brain disposition
topic Review Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3276770/
https://www.ncbi.nlm.nih.gov/pubmed/22193538
http://dx.doi.org/10.1007/s11011-011-9274-6
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