Opioid receptors: toward separation of analgesic from undesirable effects

Trends Biochem Sci. 2013 Jun;38(6):275-82. doi: 10.1016/j.tibs.2013.03.003. Epub 2013 Apr 16.

Abstract

The use of opioid analgesics for pain has always been hampered by their many side effects; in particular, the addictive liability associated with chronic use. Recently, attempts to develop analgesic agents with reduced side effects have targeted either the putative opioid receptor splice variants or the receptor hetero-oligomers. This review discusses the potential for receptor splice variant- and the hetero-oligomer-based discovery of new opioid analgesics. We also examine an alternative approach of using receptor mutants for pain management. Finally, we discuss the role of the biased agonism observed and the recently reported opioid receptor crystal structures in guiding the future development of opioid analgesics.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Alternative Splicing
  • Analgesics / pharmacology*
  • Dimerization
  • Receptors, Opioid / chemistry*
  • Receptors, Opioid / drug effects
  • Receptors, Opioid / genetics

Substances

  • Analgesics
  • Receptors, Opioid