METHODOLOGICAL ASPECTS FOR IN VITRO CHARACTERIZATION OF RECEPTOR BINDING USING C-11-LABELED RECEPTOR LIGANDS - A DETAILED STUDY WITH THE BENZODIAZEPINE RECEPTOR ANTAGONIST [C-11]RO 15-1788

摘要

As a complement to in vivo studies with positron emission tomography (PET), it is desirable to perform in vitro characterization of newly developed C-11 tracers. In this report we describe the technique for determination of receptor-ligand kinetics utilizing ligands labeled with the short lived radionuclide C-11. The limitations and advantages are discussed. The benzodiazepine antagonist [C-11]Ro 15-1788 was used as a model substance, and the use of storage phosphor plates for quantification of radioactivity was validated, Storage phosphor plates showed an excellent linear range (similar to 10(3)) and acceptable resolution (similar to 0.5 mm). Receptor-ligand kinetics, including depletion, association and dissociation, saturation and displacement were evaluated with good results through the use of short lived radiotracers and storage phosphor plates. (C) 1997 Elsevier Science Inc. [References: 33]