alexa Towards a Thermodynamic Definition of Efficacy in Partial Agonism: I Concentration-Response Theory for Explicit Agonist and Antagonist Complexes

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Towards a Thermodynamic Definition of Efficacy in Partial Agonism: I Concentration-Response Theory for Explicit Agonist and Antagonist Complexes

The pharmacological characteristics of a partial agonist, namely its binding and efficacy, are transposed, here, to give more insight into the mode of binding of the requisite agonist and antagonist bound complexes. Simple proportionality relationships of the efficacy to the overall binding define the agonist and antagonist binding constants. The advantage of such description lies in determining the thermodynamic profiles of the respective complexes by simple temperature variation. The enthalpic difference between agonist and antagonist complexes becomes a function of the efficacy, e alone, the thermodynamic scale ratio, e / (1-e), yielding this value directly.

Broadley KJ, Sykes SC, Davies RH (2010) Towards a Thermodynamic Definition of Efficacy in Partial Agonism: I Concentration-Response Theory for Explicit Agonist and Antagonist Complexes. J Thermodyn Catal 1:102. doi: 10.4172/2157-7544.1000102

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