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 tri...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.展开更多
基金Supported by the National Natural Science Foundation of China(Grant No.20771011and21071010)
文摘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.
