V. Calderone et E. Martinotti, A simplified empirical approach to evaluate the dissociation constant of afull agonist by the irreversible receptor inactivation method, J PHARM TOX, 40(1), 1998, pp. 57-62
Citations number
22
Categorie Soggetti
Pharmacology & Toxicology
Journal title
JOURNAL OF PHARMACOLOGICAL AND TOXICOLOGICAL METHODS
The estimation of the dissociation constant (Ka) of full agonists represent
s an essential tool for the classification of drugs and drug receptors, in
functional pharmacology. The evaluation of the Ka was a problem until the d
evelopment of the Furchgott's method (irreversible partial receptor inactiv
ation method), which surely represents the most used analysis for the evalu
ation of the agonist Ka in experimental protocols on isolated tissues. The
Furchgott's method can furnish a reliable estimation of the Ka, but it requ
ires a relatively complicated manipulation of experimental data. In this ar
ticle, an alternative approach for the evaluation of the Ka is proposed, on
the basis of empirical considerations. This method, also based on the part
ial alkylation of a fraction of receptors, needs only the knowledge of the
location parameters of the concentration-response curves and the applicatio
n of a very simple equation, without any complicated intermediate interpola
tion of the experimental data. (C) 1999 Elsevier Science Inc.