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Author (up) David Roche; Debora Gil; Jesus Giraldo edit  url
doi  openurl
  Title Multiple active receptor conformation, agonist efficacy and maximum effect of the system: the conformation-based operational model of agonism, Type Journal Article
  Year 2013 Publication Drug Discovery Today Abbreviated Journal DDT  
  Volume 18 Issue 7-8 Pages 365-371  
  Abstract The operational model of agonism assumes that the maximum effect a particular receptor system can achieve (the Em parameter) is fixed. Em estimates are above but close to the asymptotic maximum effects of endogenous agonists. The concept of Em is contradicted by superagonists and those positive allosteric modulators that significantly increase the maximum effect of endogenous agonists. An extension of the operational model is proposed that assumes that the Em parameter does not necessarily have a single value for a receptor system but has multiple values associated to multiple active receptor conformations. The model provides a mechanistic link between active receptor conformation and agonist efficacy, which can be useful for the analysis of agonist response under different receptor scenarios.  
  Corporate Author Thesis  
  Publisher Elsevier Place of Publication Editor  
  Language Summary Language Original Title  
  Series Editor Series Title Abbreviated Series Title  
  Series Volume Series Issue Edition  
  ISSN ISBN Medium  
  Area Expedition Conference  
  Notes IAM; 600.057; 600.054 Approved no  
  Call Number IAM @ iam @ RGG2013a Serial 2190  
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