Abstract
This chapter will consider efficacy, the property of a molecule that changes the behavior of a receptor towards its host. It will be seen that efficacy can be positive or negative and that the manifestation of efficacy can change in accordance with the set point of the receptor system. The chapter will be divided into two main themes. The first will review the molecular mechanisms of efficacy. The second will consider the operational methods available to measure the relative efficacy of agonists and will describe a new method whereby relative efficacy estimates can be extended to predict agonist selectivity in vivo.
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Kenakin, T. (2000). Efficacy: Molecular Mechanisms and Operational Methods of Measurement. A New Algorithm for the Prediction of Side Effects. In: Kenakin, T., Angus, J.A. (eds) The Pharmacology of Functional, Biochemical, and Recombinant Receptor Systems. Handbook of Experimental Pharmacology, vol 148. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-57081-0_8
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DOI: https://doi.org/10.1007/978-3-642-57081-0_8
Publisher Name: Springer, Berlin, Heidelberg
Print ISBN: 978-3-642-63028-6
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