Synthesis of para-[18F]Fluorofenbufen Octylamide for PET Imaging of Brain Tumors: PET Imaging of Brain Tumors

Glioma is a brain tumor associated with a poor therapeutic outcome with an average life expectancy of 14months. Cyclooxygenase-2 (COX-2) expression is associated with the progression of the tumor and is considered a therapeutic target of chemo agents. Para-[F-18]Fluorofenbufen octylamide ([F-18]FFOA) was obtained with the radiochemical yield of 16% and specific activity of 4GBq/mol, and the IC50 values of COX-1 and COX-2 were 26.5 and 32.7 M, respectively. The stability of cold FFOA in plasma was significantly improved with a half-life of 30min, and the uptake ratio of [F-18]FFOA in rats with brain tumor was 1.5 as determined from accumulation of 3.9% injection dose (ID/g) in the brain tumor and 2.5% ID/g in the brain. [F-18]FFOA with COX-2 micromolar affinity can be used to differentiate between brain tumor and normal region.