Preparation and Biodistribution of Technetium-99m-Labeled Bis-Misonidazole (MISO) as an Imaging Agent for Tumour Hypoxia.
MEDICINAL CHEMISTRY(2015)
摘要
Diagnosis of tumour hypoxia is an important aspect in determining the course of tumour therapy. In this study, we developed a novel imaging agent, Tc-99m-ethylenedicysteine-bis-misonidazole (Tc-99m-EC-MISO), for diagnosing tumour hypoxia. We used 2-nitroimidazole as a reactant to synthesize the amino derivative of misonidazole (MISO) in the first step and then conjugated the di-amino derivative of MISO to the chelating agent ethylenedicysteine (EC) for labelling Tc-99m in the second step. Tc-99m-pertechnetate ((TcO4-)-Tc-99m) was reduced by tin chloride (SnCl2) for radio-labeling. The radiochemical purity was up to 94%. Tissue biodistribution and SPECT/CT imaging studies were conducted on subcutaneous gliomal tumour-bearing mice. The tumour-to-muscle ratio in the Tc-99m-EC-MISO group increased with time, up to 4.6 at 4 h after injection. SPECT/CT imaging confirmed that the tumours could be visualized clearly with Tc-99m-EC-MISO at 2 h. By introducing a second 2-nitroimidazole redox centre, an apparent hypoxic accumulation of this novel 99mTc-labeled imaging agent in the Tumour was observed.
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关键词
Tumour hypoxia,imaging agent,misonidazole (MISO),technetium-99m-labeled
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