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

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 a...

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Bibliographic Details
Published inBritish journal of pharmacology Vol. 180; no. 7; pp. 975 - 993
Main Authors Varga, Balazs R., Streicher, John M., Majumdar, Susruta
Format Journal Article
LanguageEnglish
Published England Blackwell Publishing Ltd 01.04.2023
Subjects
Addictions
Allosteric properties
Alternative splicing
Analgesics
Analgesics, Opioid - adverse effects
Drug-Related Side Effects and Adverse Reactions
Humans
Opioid receptors
Pain - chemically induced
Pain - drug therapy
Receptors, Opioid, mu
Respiratory Insufficiency - chemically induced
Side effects
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Summary: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
Bibliography:Funding information
University of Arizona; Arizona Biomedical Research Commission, Grant/Award Number: ADHS18‐198875; University of Health Sciences and Pharmacy in St. Louis; Center for Clinical Pharmacology, Washington University in St. Louis; National Institutes of Health, Grant/Award Numbers: UG3DA047717, R21DA044509, DA038635‐S1, R01DA038635, R01NS091238, DA046487, DA045884
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SourceType-Scholarly Journals-1
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ObjectType-Review-2
ISSN:0007-1188
1476-5381
DOI:10.1111/bph.15760