Strategies towards safer opioid analgesics-A review of old and upcoming targets

Br J Pharmacol. 2023 Apr;180(7):975-993. doi: 10.1111/bph.15760. Epub 2022 Jan 21.

Abstract

Opioids continue to be of use for the treatment of pain. Most clinically used analgesics target the μ opioid receptor whose activation results in adverse effects like respiratory depression, addiction and abuse liability. Various approaches have been used by the field to separate receptor-mediated analgesic actions from adverse effects. These include biased agonism, opioids targeting multiple receptors, allosteric modulators, heteromers and splice variants of the μ receptor. This review will focus on the current status of the field and some upcoming targets of interest that may lead to a safer next generation of analgesics. LINKED ARTICLES: This article is part of a themed issue on Advances in Opioid Pharmacology at the Time of the Opioid Epidemic. To view the other articles in this section visit http://onlinelibrary.wiley.com/doi/10.1111/bph.v180.7/issuetoc.

Publication types

  • Review
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics, Opioid / adverse effects
  • Drug-Related Side Effects and Adverse Reactions*
  • Humans
  • Pain / chemically induced
  • Pain / drug therapy
  • Receptors, Opioid, mu
  • Respiratory Insufficiency* / chemically induced

Substances

  • Analgesics, Opioid
  • Receptors, Opioid, mu