Preparation and evaluation of ethyl [(18)F]fluoroacetate as a proradiotracer of [(18)F]fluoroacetate for the measurement of glial metabolism by PET.

Introduction: Changes in glial metabolism in brain ischemia, Alzheimer's disease, depression, schizophrenia, epilepsy and manganese neurotoxicity have been reported in recent studies. Therefore, it is very important to measure glial metabolism in vivo for the elucidation and diagnosis of these diseases. Radiolabeled acetate is a good candidate for this purpose, but acetate has little uptake in the brain due to its low lipophilicity.

New approach to fully automated synthesis of sodium [18F]fluoroacetate -- a simple and fast method using a commercial synthesizer.

A simple, rapid and fully automated preparation of sodium [(18)F]fluoroacetate has been developed by taking advantage of the similarities between the reaction pathways of [(18)F]fluoroacetate and [(18)F]-2-fluoro-deoxyglucose (FDG). The automated synthesis of sodium [(18)F]fluoroacetate was achieved with a commercial [(18)F]FDG synthesizer, the TRACERlab MX(FDG). The method produced the desired compound in a short synthesis time (32 min) and with a high and reproducible radiochemical yield (50.