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    羰基锝硝基咪唑化合物99Tcm(CO)3-MNLS的标记和生物学评价

    Preparation and Evaluation of a Novel Hypoxic Imaging Agent 99Tcm(CO)3-MNLS

      摘要
    • 摘要: 本文采用直接标记法在水相中将羰基锝中间体［99Tcm(CO)3(H2O)3］+与含磷酸基团的硝基咪唑衍生物2-(2-甲基-5-硝基咪唑-1-基)乙基磷酸盐(2-(2-methyl-5-nitro-1H-imidazol-1-yl) ethyl dihydrogen phosphate, MNLS）配位得到99Tcm(CO)3-MNLS配合物；研究了99Tcm(CO)3-MNLS的最佳标记条件、理化性质及其在荷EMT-6肿瘤小鼠体内的生物分布。结果表明，当MNLS质量为10mg、pH=4.0～8.0、80℃下反应15 min时，99Tcm(CO)3-MNLS配合物放化纯度大于99%。电泳试验结果提示，99Tcm(CO)3-MNLS为水溶性的电中性配合物，具有良好的体外稳定性。动物分布试验显示，99Tcm(CO)3-MNLS在荷EMT-6肿瘤小鼠体内有较高的肿瘤摄取值，且滞留较好；此外，99Tcm(CO)3-MNLS较99Tcm-MNLS在骨中的摄取值明显降低。以上结果为研发新型乏氧组织显像剂提供了重要参考。

       

      Abstract: The labeling method for 99Tcm(CO)3-MNLS was established, and the biodistribution of 99Tcm(CO)3-MNLS in EMT-6 tumor-bearing mice was carried out as well. The optimal labeling condition was found as follows: MNLS 10 mg, pH=4.0-8.0 at 80℃ for 15 min; and the radiochemical purity was more than 99% proved by HPLC. The new radiolabeled compound’s stability was good in vitro, and it was electrically neutral and water-soluble. The biodistribution in EMT-6 tumor-bearing mice show that: 99Tcm(CO)3-MNLS has a considerable uptake and eligible retention time in tumor, and the bone uptake of 99Tcm(CO)3-MNLS is much lower than 99Tcm-MNLS.

       

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