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Ligand bias at the μ-opioid receptor.
MedLine Citation:
PMID:  23356286     Owner:  NLM     Status:  In-Data-Review    
Abstract/OtherAbstract:
Ligand bias refers to the ability of a drug at a receptor to activate selectively particular cell signalling pathways over others, in a way that cannot be explained by traditional models of receptor theory. For a physiologically and therapeutically important GPCR (G-protein-coupled receptor) such as the MOPr (μ-opioid receptor), the role of ligand bias is currently being explored, not only in order to understand the molecular function of this receptor, but also with a view to developing better analgesic drugs with fewer adverse effects. In this short review, the ways to detect and quantify agonist bias at MOPr are discussed, along with the possible significance of MOPr ligand bias in the therapeutic use of opioid drugs. An important conclusion of this work is that attempts to define ligand bias at any GPCR on the basis of the visual inspection of concentration-response curves or comparison of maximum response (Emax) values can be misleading. Instead, reliable estimations of relative agonist efficacy are needed to calculate bias effectively.
Authors:
Eamonn Kelly
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  Biochemical Society transactions     Volume:  41     ISSN:  1470-8752     ISO Abbreviation:  Biochem. Soc. Trans.     Publication Date:  2013 Feb 
Date Detail:
Created Date:  2013-01-29     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  7506897     Medline TA:  Biochem Soc Trans     Country:  England    
Other Details:
Languages:  eng     Pagination:  218-24     Citation Subset:  IM    
Affiliation:
School of Physiology and Pharmacology, University of Bristol, Bristol BS8 1TD, U.K.
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