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Author (up) David Roche; Debora Gil; Jesus Giraldo edit  doi
  Title Mechanistic analysis of the function of agonists and allosteric modulators: Reconciling two-state and operational models Type Journal Article
  Year 2013 Publication British Journal of Pharmacology Abbreviated Journal BJP  
  Volume 169 Issue 6 Pages 1189-202  
  Abstract Two-state and operational models of both agonism and allosterism are compared to identify and characterize common pharmacological parameters. To account for the receptor-dependent basal response, constitutive receptor activity is considered in the operational models. By arranging two-state models as the fraction of active receptors and operational models as the fractional response relative to the maximum effect of the system, a one-by-one correspondence between parameters is found. The comparative analysis allows a better understanding of complex allosteric interactions. In particular, the inclusion of constitutive receptor activity in the operational model of allosterism allows the characterization of modulators able to lower the basal response of the system; that is, allosteric modulators with negative intrinsic efficacy. Theoretical simulations and overall goodness of fit of the models to simulated data suggest that it is feasible to apply the models to experimental data and constitute one step forward in receptor theory formalism.  
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  Notes IAM; 600.044; 605.203 Approved no  
  Call Number IAM @ iam @ RGG2013b Serial 2195  
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