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      Opioid receptors: toward separation of analgesic from undesirable effects.

      1 , ,

      Trends in biochemical sciences

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          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.

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          Author and article information

          Journal
          Trends Biochem. Sci.
          Trends in biochemical sciences
          0968-0004
          0968-0004
          Jun 2013
          : 38
          : 6
          Affiliations
          [1 ] Department of Pharmacology, University of Minnesota, Medical School, Minneapolis, MN 55455, USA. lawxx001@umn.edu
          Article
          S0968-0004(13)00046-7 NIHMS458990
          10.1016/j.tibs.2013.03.003
          3665630
          23598157
          Copyright © 2013 Elsevier Ltd. All rights reserved.

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