The estimation of the dissociation constant (Ka) of full agonists represents an essential tool for the classification of drugs and drug receptors, in functional pharmacology. The evaluation of the Ka was a problem until the development of the Furchgott's method (irreversible partial receptor inactivation method), which surely represents the most used analysis for the evaluation of the agonist Ka in experimental protocols on isolated tissues. The Furchgott's method can furnish a reliable estimation of the Ka, but it requires a relatively complicated manipulation of experimental data. In this article, an alternative approach for the evaluation of the Ka is proposed, on the basis of empirical considerations. This method, also based on the partial alkylation of a fraction of receptors, needs only the knowledge of the location parameters of the concentration-response curves and the application of a very simple equation, without any complicated intermediate interpolation of the experimental data.
A simplified empirical approach to evaluate the dissociation constant of a full agonist by the irreversible receptor inactivation method
CALDERONE, VINCENZO;
1998-01-01
Abstract
The estimation of the dissociation constant (Ka) of full agonists represents an essential tool for the classification of drugs and drug receptors, in functional pharmacology. The evaluation of the Ka was a problem until the development of the Furchgott's method (irreversible partial receptor inactivation method), which surely represents the most used analysis for the evaluation of the agonist Ka in experimental protocols on isolated tissues. The Furchgott's method can furnish a reliable estimation of the Ka, but it requires a relatively complicated manipulation of experimental data. In this article, an alternative approach for the evaluation of the Ka is proposed, on the basis of empirical considerations. This method, also based on the partial alkylation of a fraction of receptors, needs only the knowledge of the location parameters of the concentration-response curves and the application of a very simple equation, without any complicated intermediate interpolation of the experimental data.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
