~(99)Tc~m-MAG_2-Ade肿瘤显像剂的合成及其生物活性研究

    Synthesis and Biodistribution of ~(99)Tc~m-MAG_2-Ade as A Tumor Imaging Agent

    • 摘要: 为了制备肿瘤显像剂99Tcm标记肽,合成并表征了新的碱基修饰的小肽配体9-N-(S-三苯甲基巯基乙酰)二甘氨酰氨基乙基腺嘌呤(Tr-MAG2-Ade)。通过直接标记法得到了水溶性配合物99Tcm-MAG2-Ade,并对其体外稳定性进行了检测。在荷瘤小鼠体内的生物分布结果表明,99Tcm-MAG2-Ade在肿瘤中有较高的摄取,肿瘤与肌肉的摄取比为5.7,肿瘤与血液的摄取比为1.55。血液清除较快,有望用于非腹部肿瘤的显像。

       

      Abstract: A new peptide ligand containing adenine 9-N-(S-tritylmercaptoacetyl) diglycylaminoethyl adenine (Tr-MAG2-Ade) is synthesized and characterized by IR, 1H NMR, 13C NMR, MS and elemental analysis. The complex 99Tcm-MAG2-Ade is prepared by directly labeling method. The partition coefficient and stability in vitro indicated that the complex is hydrophilic and stable over a period of 6 h at room temperature. The biodistribution of 99Tcm-MAG2-Ade in mice bearing S180 tumor shows that a tumor-specific accumulation and quick blood clearance. The uptake ratios of tumor to muscle and blood at 3 hours post injection are 5.70 and 1.55, respectively. The complex 99Tcm-MAG2-Ade appears to be a potential tumor imaging agent.

       

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