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

RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE

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

MEI Lei，

CHU Taiwei

Nuclear Science and Techniques

Vol.22, No.2

pp.105-110

Published in print 20 Apr 2011

DOI：10.13538/j.1001-8042/nst.22.105-110

28500

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 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 ^99mTc(CO)₃-His-NI has a potential to image tumor hypoxia.

TumorHypoxia4-nitroimidazole[99mTc(CO)3(H2O)3]+Histidine

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