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Mu opioid receptor antagonists: recent developments.

Allan J Goodman1, Bertrand Le Bourdonnec, Roland E Dolle

  • 1Department of Medicinal Chemistry, Adolor Corporation, 700 Pennsylvania Drive, Exton, PA 19341, USA. agoodman@adolor.com

Chemmedchem
|October 9, 2007
PubMed
Summary
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Mu opioid antagonists offer pain relief with fewer side effects like dependence. New peripherally restricted compounds show promise for treating various conditions without affecting central pain management.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry

Background:

  • Mu opioid agonists (e.g., morphine) are primary analgesics but cause severe side effects.
  • Current antagonists (naloxone, naltrexone) treat adverse effects but have limitations.

Purpose of the Study:

  • To discuss structural classes of mu opioid antagonists.
  • To explore potential clinical applications beyond current uses.
  • To review recent patents in the field.

Main Methods:

  • Literature review of mu opioid antagonists.
  • Analysis of structural classes and properties.
  • Review of patents filed in the last decade.

Main Results:

  • Identification of various structural classes of mu opioid antagonists.

Related Experiment Videos

  • Exploration of therapeutic potential in pruritus, obesity, and tardive dyskinesia.
  • Highlighting peripherally restricted antagonists (N-methylnaltrexone, alvimopan) for targeted side effect management.
  • Conclusions:

    • Mu opioid receptor antagonism has broad therapeutic potential.
    • Peripherally restricted antagonists offer a promising approach to manage opioid-induced side effects without compromising analgesia.
    • Ongoing research and patent activity indicate a dynamic field.