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 ›› 2011, Vol. 22 ›› Issue (2): 105-110 doi: 10.13538/j.1001-8042/nst.22.105-110

• RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICIN • Previous Articles     Next Articles

[(99m)Tc(CO)_3]+ labeled histidine derivative containing 4-nitroimidazole:Synthesis,biodistribution as a tumor hypoxia imaging agent

MEI Lei CHU Taiwei   

  1. Beijing National Laboratory for Molecular Sciences,Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science,College of Chemistry and Molecular Engineering,Peking University,Beijing 100871,China
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MEI Lei, CHU Taiwei. [(99m)Tc(CO)_3]+ labeled histidine derivative containing 4-nitroimidazole:Synthesis,biodistribution as a tumor hypoxia imaging agent.Nuclear Science and Techniques, 2011, 22(2): 105-110     doi: 10.13538/j.1001-8042/nst.22.105-110

Abstract:

A novel histidine derivative containing 4-nitroimidazole,(S)-2-(4-((4-nitro-1H-imidazol-1-yl) methyl) benzamido)-3-(1H-imidazol-4-yl)propanoic acid (His-NI),was synthesized and labeled with [99mTc(CO)3(H2O)3]+.The tricarbonyl technetium complex,the 99mTc(CO)3-His-NI,showed a 99% yield under mild conditions at a low His-NI ligand concentration of 10-4 molL-1,and its biodistribution in mice bearing S180 tumor had a selective accumulation in tumor (2.01±0.40%ID/g at 1 h postinjection) and a slow clearance.The tumor/muscle ratio was 1.64 at 1 h,3.10 at 4 h,and 3.88 at 24 h,indicating that the 99mTc(CO)3-His-NI has a potential to image tumor hypoxia.

Key words: Tumor, Hypoxia, 4-nitroimidazole, [99mTc(CO)3(H2O)3]+, Histidine