Radiofluorination of PSMA-HBED via (AlF2+)-F-18 Chelation and Biological Evaluations In Vitro

摘要

Ga-68-labeled prostate-specific membrane antigen (PSMA) ligands have been used clinically for positron emission tomography (PET) imaging of prostate cancer. However, F-18-labeled compounds offer several advantages, including the potential for delayed imaging, high starting activities enabling multidose preparation, and improved spatial resolution in PET. For F-18 labeling of peptides conjugated with a suitable chelator, a fast and feasible method is the use of [(AlF)-F-18](2+). In the present study, the radiofluorinations of a well-known PSMA ligand Glu-NH-CO-NH-Lys(Ahx)-HBED-CC (PSMA-HBED) via [(AlF)-F-18](2+) were performed with respect to various reaction parameters, along with the biological evaluations in a cell experiment.