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The interaction of a drug with a receptor generates a code of
information having components of affinity and efficacy. How this
information is translated into a response depends on the unique
cells, tissue, organ or system in which the receptor resides. This
book describes how to analyze various responses to estimate the
affinity and efficacy components of the initial drug-receptor
interaction. More specifically, it describes how to measure the
affinity and efficacy of drugs through the analysis of single
receptor activity, the activation state of a population of
receptors, and responses downstream from receptor activation. More
light is thrown on ligand-gated ion channels and G protein-coupled
receptors in this book.The topics discussed include radioligand
binding, estimation of agonist affinity and efficacy, competitive
antagonism, inverse agonism, allosteric agonists and modulators,
agonist bias, modulation of pathway selectivity, and the estimation
of ligand affinity for active and inactive receptor states. The
natural history and structure of ligand-gated ion channels, G
proteins, and G protein-coupled receptors are also discussed.
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