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Bulletin of the Korean Chemical Society v.26 no.1, 2005년, pp.91 - 96   피인용횟수: 3

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

Moon, Byung-Seok    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences   ); Kim, Sang-Wook    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences   ); Lee, Tae-Sup    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences   ); Ahn, Soon-Hyuk    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences   ); Lee, Kyo-Chul    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences   ); An, Gwang-Il    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences   ); Yang, Seung-Dae    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences   ); Chi, Dae-Yoon    (Department of Chemistry, Inha University   ); Choi, Chang-Woon    (Department of Nuclear Medicine, Korea Institute of Radiological and Medical Sciences   ); Lim, Sang-Moo    (Department of Nuclear Medicine, Korea Institute of Radiological and Medical Sciences   ); Chun, Kwon-Soo    (Laboratory of Cyclotron Application, Korea Institute of Radiological and Medical Sciences  );
  • 초록

    O-(3-[ $^{18}$ F]Fluoropropyl)-L-tyrosine (L-[ $^{18}$ F]FPT) was synthesized by nucleophilic radiofluorination followed by acidic hydrolysis of protective groups and evaluated with 9 L tumor bearing rat. L-[ $^{18}$ F]FPT is an homologue of O-(2-[ $^{18}$ F]fluoroethyl)-L-tyrosine (L-[ $^{18}$ F]FET) which recently is studied as a tracer for tumor imaging using positron emission tomography (PET). [ $^{18}$ F]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 [ $^{18}$ F]FPT was 0-45% (decay corrected) and the radiochemical purity was more than 95% after HPLC purification. The total time elapsed for the synthesis of [ $^{18}$ F]FPT was 100 min from EOB (End-of-bombardment). A comparison of uptake studies between [ $^{18}$ F]FPT and [ $^{18}$ F]FET was performed. In biodistribution, [ $^{18}$ F]FPT showed similar pattern with [ $^{18}$ F]FET in various tissues, but [ $^{18}$ F]FPT showed low uptake in brain. Furthermore, [ $^{18}$ F]FPT showed higher tumor-to-brain ratio than [ $^{18}$ F]FET. In conclusion, [ $^{18}$ F]FPT seems to be more useful amino acid tracer than [ $^{18}$ F]FET for brain tumors imaging with PET.


  • 주제어

    O-(3-[ $^{18}$F]Fluoropropyl)-L-tyrosine (L-[ $^{18}$F]FPT) .   O-(2-[ $^{18}$F]Fluoroethyl)-L-tyrosine (L-[ $^{18}$F]FET) .   Tumor imaging .   PET.  

  • 참고문헌 (18)

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  • 이 논문을 인용한 문헌 (3)

    1. 2005. "" Bulletin of the Korean Chemical Society, 26(4): 599~602     
    2. 2006. "" Bulletin of the Korean Chemical Society, 27(8): 1203~1205     
    3. Shim, Ah-Young ; Moon, Byung-Seok ; Lee, Tae-Sup ; Lee, Kyo-Chul ; An, Gwang-Il ; Yang, Seung-Dae ; Yu, Kook-Hyun ; Cheon, Gi-Jeong ; Choi, Chang-Woon ; Lim, Sang-Moo ; Chun, Kwon-Soo 2006. "A Study on Preparation of 3'-$[^{18}F]$Fluoro-3'-deoxythymidine and Its Biodistribution in 9L Glioma Bearing Rats" 핵의학 분자영상 = Nuclear medicine and molecular imaging, 40(5): 263~270     

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