Functional methods for quantifying agonists and antagonists

• Published in: Journal of receptors and signal transduction Vol. 21; no. 2-3; p. 117
• Main Author: Dougall, L G
• Format: Journal Article
• Language: English
• Published: England 2001
• Subjects: Animals; Binding Sites; Drug Antagonism; Humans; Models, Theoretical; Pharmacology - methods; Receptors, Drug - agonists; Receptors, Drug - antagonists & inhibitors
• DOI: 10.1081/RRS-100107425
• ISSN: 1079-9893

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.