Effects of Contamination on Radioligand Binding Parameters

Radioligand binding studies are used to provide quantitative estimates of parameters such as the receptor density of a tissue and the affinity values of labelled and unlabelled ligands. The presence of an unlabelled competing contaminant, which might be present because of actual contamination, inadequate radioligand purification or the breakdown of the radioligand to an active species, has surprising effects on these estimates: the apparent affinity of the radioligand is increased but the Ki values of unlabelled ligands are unaffected. The most striking and sensitive effects are on radioligand association kinetics, which become independent of radioligand concentration at high radioligand concentrations.