title: Opioid receptors: toward separation of analgesic from undesirable effects.
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.
authors.affiliation: Department of Pharmacology, University of Minnesota, Medical School, Minneapolis, MN 55455, USA. lawxx001@umn.edu
authors.forename: Ping-Yee
authors.initials: PY
authors.lastname: Law
authors.forename: Patricia H
authors.initials: PH
authors.lastname: Reggio
authors.forename: Horace H
authors.initials: HH
authors.lastname: Loh
mesh_terms: D017398:Alternative Splicing; D000700:Analgesics / Q000494:pharmacology*; D019281:Dimerization; D011957:Receptors, Opioid / Q000737:chemistry* / Q000187:drug effects / Q000235:genetics
chemical_list: D000700:Analgesics; D011957:Receptors, Opioid