The quantification of relative efficacy of agonists.
While much pharmacological effort has been expended in the measurement, quantification, and comparison of agonist affinity for the classification of drugs and drug receptors, inordinately less emphasis has been placed on the quantification of the other property of agonists, namely intrinsic efficacy. This is unfortunate as the existing studies of the relative intrinsic efficacy of agonists show this to be a most useful scale for the classification of agonists and the prediction of tissue responses. This paper will review some of the theories that describe efficacy on a molecular level, the methods of measuring relative efficacy, and the factors in these procedures which can lead to artifacts and misleading information for the classification of drug receptors. Lastly, the value of the quantification of efficacy will be discussed in terms of the design of agonists for therapeutic advantage.
Kenakin
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D000818:Animals; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007700:Kinetics; D011956:Receptors, Cell Surface / Q000187:drug effects* / Q000378:metabolism; D011955:Receptors, Drug / Q000187:drug effects* / Q000378:metabolism
D011956:Receptors, Cell Surface; D011955:Receptors, Drug