[Tc-99m(CO)(3)]( ) labeled histidine derivative containing 4-nitroimidazole: Synthesis, biodistribution as a tumor hypoxia imaging agent

作者：Me Lei; Chu Taiwei^*

来源：Nuclear Science and Techniques, 2011, 22(2): 105-110.

• Tumor
• Hypoxia
• 4-nitroimidazole
• [Tc-99m(CO)(3)(H2O)(3)]( )
• Histidine

A novel histidine derivative containing 4-nitroimidazole, (S)-2-(4-((4-nitro-1H-imidazol-l-yl) methyl) benzamido) -3- (1H- imidazol-4-yl)propanoic acid (His-NI), was synthesized and labeled with [Tc-99m(CO)(3)(H2O)(3)](+). The tricarbonyl technetium complex, the Tc-99m(CO)(3)-His-NI, showed a 99% yield under mild conditions at a low His-NI ligand concentration of 10(-4) mol.L-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 Tc-99m(CO)(3)-His-NI has a potential to image tumor hypoxia.

• 出版日期2011-4
• 单位北京大学