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A critical appraisal of intrinsic activity, efficacy and intrinsic efficacy with reference to the development and the current meaning / Karen KrügerKruger, Karen January 2006 (has links)
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.
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A critical appraisal of intrinsic activity, efficacy and intrinsic efficacy with reference to the development and the current meaning / Karen KrügerKruger, Karen January 2006 (has links)
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.
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