Mu opioid receptor antagonists: Recent developments

Allan J. Goodman, Bertrand Le Bourdonnec, Roland E. Dolle

Research output: Contribution to journalReview articlepeer-review

70 Scopus citations


For thousands of years mu opioid agonists such as morphine have been utilized for their analgesic properties. Today, morphine and related compounds are still used as a first line therapy in the treatment of mode rate to severe pain. However, despite the clear benefits of mu agonists in pain management, severe side effects such as dependence and respiratory depression are associated with use of these drugs. To date, there are only two approved mu opioid antagonists for use in the treatment of these adverse effects, that is, naloxone and naltrexone. However, many other clinical and therapeutic areas have been linked to mu opioid receptor antagonism. These include treatment of opioid induced pruritis of the skin, obesity, and Parkinson-induced tardive dyskinesia. Currently there are two compounds, N-methylnaltrexone and alvimopan, under FDA review as possible treatments for opioid induced bowel dysfunction and postoperative ileus. These compounds are ofspecial interest as they are peripherally restricted. This attribute enables treatment of peripheral side effects induced by opioid agonists without reversal of the centrally mediated analgesia ofthe agonist. In this article we discuss the structural classes of mu opioid antagonists, their potential clinical applications, and review the relevant patents of the last ten years.

Original languageEnglish
Pages (from-to)1552-1570
Number of pages19
Issue number11
StatePublished - Nov 12 2007


  • Opioids
  • Receptors
  • mu agonists
  • mu antagonists


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