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.
Original language | English (US) |
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Pages (from-to) | 275-282 |
Number of pages | 8 |
Journal | Trends in Biochemical Sciences |
Volume | 38 |
Issue number | 6 |
DOIs | |
State | Published - Jun 2013 |
Bibliographical note
Funding Information:This work is supported in parts by National Institute on Drug Abuse (NIDA) grants DA023905 (P.Y.L.), DA031442 (P.Y.L.), DA000564 (H.H.L.), DA011806 (H.H.L.), and K05 DA021358 (P.H.R.).
Keywords
- Hetero-oligomers
- Receptor mutants as therapeutic targets
- Receptor splice variants