A critical appraisal of intrinsic activity, efficacy and intrinsic efficacy with reference to the development and the current meaning / Karen Krüger

• Main Author: Kruger, Karen
• Published: North-West University 2009
• Subjects: Agonist activity; Conformational change; Drug-receptor interaction; Efficacy; Intrinsic activity; Intrinsic efficacy; Occupation model; Operational model; Ternary complex model; Two-state model
• Online Access: http://hdl.handle.net/10394/1088

It has been observed that confusion exists in literature concerning the meaning and use of the term efficacy. Confusion is worsened by the use of the term as a general term describing agonist activity. The meaning of the terms intrinsic activity, efficacy and intrinsic efficacy as used in theoretical models of drug action was investigated. The classical occupation model, the two-state model, the ternary complex model (including conformational change and ideas surrounding G-proteins) and the operational model were studied in order to understand the historical and current usage of these terms. Although efficacy estimates are often reported as a molecular property, it was shown that agonist activity is tissue dependent and cannot be fully portrayed by an efficacy estimate. It was found that efficacy has a different definition in each model. This is not always recognized in literature. It was suggested that the term efficacy should only be used in the context of a specific model === Thesis (M.Sc. (Pharmacology))--North-West University, Potchefstroom Campus, 2007.