Synthesis of O-(3-[18F]Fluoropropyl)-L-tyrosine (L-[18F]FPT) and Its Biological Evaluation in 9L Tumor Bearing Rat¢Ó

Bulletin of the Korean chemical society

Seung Dae Yang¹  Dae Yoon Chi¹  Sang Moo Lim¹  Gwang Il An¹  Tae Sup Lee¹  Soon Hyuk Ahn¹  Byung Seok Moon¹  Sang Wook Kim¹  Chang Woon Choi¹  Kwon Soo Chun¹  Kyo Chul Lee¹ 

关键词: O-(3-[18F]Fluoropropyl)-L-tyrosine (L-[18F]FPT);    O-(2-[18F]Fluoroethyl)-L-tyrosine (L-[18F]FET);    Tumor imaging;    PET.;   

DOI  :  

学科分类：化学（综合）

来源: Korean Chemical Society

【 摘 要 】

O-(3-[18F]Fluoropropyl)-L-tyrosine (L-[18F]FPT) was synthesized by nucleophilic radiofluorination followed by acidic hydrolysis of protective groups and evaluated with 9 L tumor bearing rat. L-[18F]FPT is an homologue of O-(2-[18F]fluoroethyl)-L-tyrosine (L-[18F]FET) which recently is studied as a tracer for tumor imaging using positron emission tomography (PET). [18F]FPT was directly prepared from the precursor of O-(3-ptoluenesulfonyloxypropyl)-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 [18F]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 [18F]FPT was 100 min from EOB (End-of-bombardment). A comparison of uptake studies between [18F]FPT and [18F]FET was performed. In biodistribution, [18F]FPT showed similar pattern with [18F]FET in various tissues, but [18F]FPT showed low uptake in brain. Furthermore, [18F]FPT showed higher tumor-to-brain ratio than [18F]FET. In conclusion, [18F]FPT seems to be more useful amino acid tracer than [18F]FET for brain tumors imaging with PET.

【 授权许可】

Unknown