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Affinity and Efficacy:The Components of Drug-Receptor by Frederick J Ehlert

By Frederick J Ehlert

The interplay of a drug with a receptor generates a code of data having elements of affinity and efficacy. How this data is translated right into a reaction depends upon the original cells, tissue, organ or approach during which the receptor is living. This ebook describes tips on how to study quite a few responses to estimate the affinity and efficacy parts of the preliminary drug–receptor interplay. extra particularly, it describes how one can degree the affinity and efficacy of substances throughout the research of unmarried receptor task, the activation nation of a inhabitants of receptors, and responses downstream from receptor activation. extra gentle is thrown on ligand-gated ion channels and G protein-coupled receptors during this book.

The subject matters mentioned comprise radioligand binding, estimation of agonist affinity and efficacy, aggressive antagonism, inverse agonism, allosteric agonists and modulators, agonist bias, modulation of pathway selectivity, and the estimation of ligand affinity for lively and inactive receptor states. The common background and constitution of ligand-gated ion channels, G proteins, and G protein-coupled receptors also are discussed.

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