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 knowledge is translated right into a reaction is determined by the original cells, tissue, organ or method within which the receptor is living. This booklet describes the right way to learn numerous responses to estimate the affinity and efficacy parts of the preliminary drug–receptor interplay. extra in particular, it describes find out how to degree the affinity and efficacy of substances in the course of the research of unmarried receptor task, the activation country 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 typical heritage and constitution of ligand-gated ion channels, G proteins, and G protein-coupled receptors also are discussed.
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Affinity and Efficacy:The Components of Drug-Receptor Interactions by Frederick J Ehlert