Abstract
O-(3-[ 1 8 F]Fluoropropyl)-L-tyrosine (L-[ 1 8 F]FAT) was synthesized by nucleophilic radiofluorination followed by acidic hydrolysis of protective groups and evaluated with 9 L tumor bearing rat. L-[ 1 8 F]FAT is an homologue of O-(2-[ 1 8 F]fluoroethyl)-L-tyrosine (L-[ 1 8 F]FET) which recently is studied as a tracer for tumor imaging using positron emission tomography (PET). [ 1 8 F]FPT was directly prepared from the precursor of O-(3-p-toluenesulfonyloxypropyl)-N-(tert-butoxycarbonyl)-L-tyrosine methyl ester. FPT-PET image was obtained at 60 min in 9 L tumor bearing rats. The radiochemical yield of [ 1 8 F]FPT was 40-45% (decay corrected) and the radiochemical purity was more than 95% after HPLC purification. The total time elapsed for the synthesis of [ 1 8 F]FPT was 100 min from EOB (End-of-bombardment). A comparison of uptake studies between [ 1 8 F]FPT and [ 1 8 F]FET was performed. In biodistribution, [ 1 8 F]FPT showed similar pattern with [ 1 8 F]FET in various tissues, but [ 1 8 F]FPT showed low uptake in brain. Furthermore, [ 1 8 F]FPT showed higher tumor-to-brain ratio than [ 1 8 F]FET. In conclusion, [ 1 8 F]FPT seems to be more useful amino acid tracer than [ 1 8 F]FET for brain tumors imaging with PET.
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