S. Lazareno et Njm. Birdsall, ESTIMATION OF ANTAGONIST-K(B) FROM INHIBITION CURVES IN FUNCTIONAL EXPERIMENTS - ALTERNATIVES TO THE CHENG-PRUSOFF EQUATION, Trends in pharmacological sciences, 14(6), 1993, pp. 237-239
Recent Principles articles have considered procedures for the function
al estimation of an antagonist's dissociation constant from the result
s of an antagonist inhibition curve in the presence of a fixed concent
ration of agonist. Leff and Dougall (TiPS 14, 110-112) have derived an
equation, analogous to the (generally invalid) Cheng-Prusoff equation
, which requires that the agonist concentration-effect curves have the
form of a logistic function. In the final article of the series, Seba
stian Lazareno and Nigel Birdsall consider this equation in the contex
t of two related methods for analysing functional inhibition curves -
a null method that makes no assumptions about the shapes of curves, an
d a curve-fitting method that provides an estimate of the antagonist S
child slope.