Nuclear Science and Techniques

《核技术》(英文版) ISSN 1001-8042 CN 31-1559/TL     2019 Impact factor 1.556

Nuclear Science and Techniques ›› 2013, Vol. 24 ›› Issue (3): 030302 doi: 10.13538/j.1001-8042/nst.2013.03.008


Study on radiolabeling of 1,2,3-triazole analogs with fac-[188Re(CO)3(H2O)3]+ via click chemistry

WANG Cheng1  YIN Jilin1  ZHOU Wei2  ZHANG Lan ZHOU Zheng1   

  1. 1PET/CT center, General Hospital of Guangzhou Military Command, Guangzhou 510010, China
    2Shanghai Institute of Applied Physics, Chinese Academy of Sciences, Jiading Campus, Shanghai 201800, China
  • Received:2013-03-28
  • Contact: YIN Jilin
  • Supported by:

    Supported by National Natural Science Foundation of China (No.10875163) and Natural Science Foundation of Guangdong Province (Nos.2009B030108036 and S2012010010685)

PDF ShareIt Export Citation
WANG Cheng, YIN Jilin, ZHOU Wei, ZHANG Lan, ZHOU Zheng. Study on radiolabeling of 1,2,3-triazole analogs with fac-[188Re(CO)3(H2O)3]+ via click chemistry.Nuclear Science and Techniques, 2013, 24(3): 030302     doi: 10.13538/j.1001-8042/nst.2013.03.008


Click chemistry was used to study on radiolabeling of 1,2,3-triazole analogs with fac-[188Re(CO)3(H2O)3]+. CuSO4/L-sodium ascorbate was chosen as the catalyst system, three terminal alkynes were conjugated with two different azides respectively, and then the new prepared fac-[188Re(CO)3(H2O)3]+ was coordinated to the six triazoles. The results showed that the radiochemical yields (RCY) of the conjugation of fac-[188Re(CO)3]+ with six triazoles were over 90%, and the triazoles showed high stability in phosphate-buffered saline and new-born calf serum. The preliminary biological evaluation results showed that the new 188Re-labeling method via click chemistry could have general application in labeling bioactive molecules in high radiochemical yield and high specific activity for further SPECT research.


Key words: TricarbonylRhenium-188, Stability, Triazole analogs, Radiotherapy, Click chemistry