^(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

作　　者：赵云岭[1] 张春丽[2] 齐传民[1] 游桂荣[1] 付占立[2] 郭凤琴[2] 王荣福[2] 

机构地区：[1]北京师范大学化学系,北京100875 [2]北京大学第一医院核医学科,北京100034

出　　处：《核化学与放射化学》2005年第2期82-86,共5页Journal of Nuclear and Radiochemistry

基　　金：国家自然科学基金资助项目(20171008和20371009);北京师范大学青年科学基金(理科)资助项目(107197)

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。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.

关 键 词：肿瘤显像剂 肽 碱基 生物分布 

分 类 号：R817[医药卫生—影像医学与核医学]