By Frederick J Ehlert
The interplay of a drug with a receptor generates a code of data having parts of affinity and efficacy. How this knowledge is translated right into a reaction is dependent upon the original cells, tissue, organ or approach within which the receptor is living. This booklet describes how one can learn quite a few responses to estimate the affinity and efficacy elements of the preliminary drug–receptor interplay. extra particularly, it describes the right way to degree the affinity and efficacy of substances during the research of unmarried receptor job, 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 themes 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 energetic and inactive receptor states. The common 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