Morphine metabolism, transport and Brain disposition

Simona De Gregori, Manuela De Gregori, Guglielmina Nadia Ranzani, Massimo Allegri, Cristina Minella, Mario Regazzi

Research output: Contribution to journalArticle


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.

Original languageEnglish
Pages (from-to)1-5
Number of pages5
JournalMetabolic Brain Disease
Issue number1
Publication statusPublished - Mar 2012


  • Blood-brain-barrier
  • Genetic variability
  • Morphine
  • Morphine-3-glucuronide
  • Morphine-6-glucuronide
  • Transport mechanisms

ASJC Scopus subject areas

  • Clinical Neurology
  • Biochemistry
  • Cellular and Molecular Neuroscience

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