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 data is translated right into a reaction depends upon the original cells, tissue, organ or process during which the receptor is living. This booklet describes how one can research a variety of responses to estimate the affinity and efficacy elements of the preliminary drug–receptor interplay. extra in particular, it describes the best way to degree the affinity and efficacy of gear in the course of the research of unmarried receptor job, the activation country of a inhabitants of receptors, and responses downstream from receptor activation. extra mild is thrown on ligand-gated ion channels and G protein-coupled receptors during this book.
The issues 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 average historical past 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