Functional methods for quantifying agonists and antagonists

The development of occupancy theory has allowed the formulation of a series of mathematical models that describe the interaction of agonists and antagonists with their receptors, in terms of affinity and efficacy. These models provide a framework for the analysis and interpretation of E/[A] curve da...

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Bibliographic Details
Published inJournal of receptors and signal transduction Vol. 21; no. 2-3; p. 117
Main Author Dougall, L G
Format Journal Article
LanguageEnglish
Published England 2001
Subjects
Animals
Binding Sites
Drug Antagonism
Humans
Models, Theoretical
Pharmacology - methods
Receptors, Drug - agonists
Receptors, Drug - antagonists & inhibitors
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Summary:The development of occupancy theory has allowed the formulation of a series of mathematical models that describe the interaction of agonists and antagonists with their receptors, in terms of affinity and efficacy. These models provide a framework for the analysis and interpretation of E/[A] curve data and have proved to be useful tools in quantitative pharmacology. Unfortunately, despite the proven utility of this approach and the widespread availability of powerful computer-based curve-fitting programs [BMDP (41), Microsoft Excel. etc.], which greatly facilitate analysis, the application of mathematical modeling remains the exception rather than the rule in pharmacological studies.
ISSN:1079-9893
DOI:10.1081/RRS-100107425