Trends in Pharmacological Sciences
PrinciplesAnalysis of competitive agonist-antagonist interactions by nonlinear regression
Abstract
The rigorous estimation of a dissociation constant (Kb) for antagonists in functional assays has been sought by pharmacologists using a variety of techniques ever since the regression method of Arunlakshana and Schild in 1959. Here, Michael Lew and James Angus describe a simplified global regression method with improved accuracy compared to Schild analysis. The method is suitable for personal computers with standard graphing and statistical software. The accuracy of the predicted pKb values and confidence intervals has been tested by comparing examples of published data, and by mathematical (bootstrap) simulations.
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The β<inf>2</inf>-adrenoceptor agonist bronchodilators terbutaline and orciprenaline are also weak α<inf>1</inf>-adrenoceptor antagonists
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Odorant Receptor Inhibition Is Fundamental to Odor Encoding
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