Receptor and binding studies

Abstract

Radioligand binding studies are an important tool to quantify and qualitatively characterize receptors and hence have become a universal tool of cardiovascular research. While radioligand binding experiments are relatively simple to perform, interpretation of the results and optimisation of the experimental settings are more complex. Several criteria must be met to consider a labelled binding site a receptor: Binding should be of high affinity, saturable, stereospecific and have a ligand recognition profile similar to that of a functional response in that tissue. A hilariously funny description of the fundamental principles of radioligand binding has been presented by Guth (1982). © Springer-Verlag Berlin Heidelberg 2005.