The Receptor As An Onoff Switch

Historically, the concept of drug receptors began as an abstract idea and continued throughout pharmacology for another 70-80 years as such. Models considering receptors essentially had drugs activate (as a switch) a black box to produce tissue response. It is useful first to consider receptors as pharmacological switches since the theories used to describe drug action in

GPCR Molecular Pharmacology and Drug Targeting: Shifting Paradigms and New Directions,

Edited by Annette Gilchrist

Copyright © 2010 John Wiley & Sons, Inc.

these systems lay the foundation for the more mechanistically driven models of receptors in use today. These ideas have formed the basis for quantitative receptor theory on which new information about the biochemistry and structure of receptors has been added. These will then be discussed in terms of specific mechanistic models of 7TM receptor function and how these assist in the quantification of drug effect.

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