By Frederick J Ehlert
The interplay of a drug with a receptor generates a code of knowledge having parts 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 e-book describes the right way to examine quite a few responses to estimate the affinity and efficacy elements of the preliminary drug–receptor interplay. extra particularly, it describes the way to degree the affinity and efficacy of gear during the research of unmarried receptor job, the activation kingdom 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 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 energetic and inactive receptor states. The ordinary background and constitution of ligand-gated ion channels, G proteins, and G protein-coupled receptors also are discussed.
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