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

• NUCLEAR CHEMISTRY,RADIOCHEMISTRY,RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

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 E-mail:yinjilinpet_ct@163.com
  • Supported by:

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

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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

Abstract:

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