^(99)Tc^(m)标记基于体内无铜点击化学的葡萄糖代谢显像剂  

^(99)Tc^(m)-labeled Glucose Metabolism Imaging Agents Based on in Vivo Copper-free Click Chemistry

作　　者：陈庆鑫 褚泰伟[1] CHEN Qingxin;CHU Taiwei(Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science,College of Chemistry and Molecular Engineering,Peking University,Beijing 100871,China)

机构地区：[1]北京大学化学与分子工程学院,放射化学与辐射化学重点学科实验室,北京100871

出　　处：《同位素》2021年第4期346-354,I0002,共10页Journal of Isotopes

基　　金：国家自然科学基金资助项目(21976008,U1967216)。

摘　　要：为了发展^(99)Tc^(m)标记的葡萄糖代谢显像剂,合成MAMA偶联的二苯并环辛炔配体和四种2-位含有叠氮基的小分子葡萄糖衍生物,依据体外点击速率实验筛选出两种可能的葡萄糖衍生物(N_(3)-DG-1和N_(3)-DG-2)。首先完成N_(3)-DG-1和N_(3)-DG-2在荷S180肿瘤小鼠体内的预着靶,再注射^(99)Tc^(m)标记的环辛炔探针进行寻靶,发生体内点击反应。动物分布实验结果表明,N_(3)-DG-2的瘤血比和瘤肉比优于N_(3)-DG-1,说明^(99)Tc^(m)标记的环辛炔探针和N_(3)-DG-2组合更适用于葡萄糖代谢显像。In order to develop an ideal^(99)Tc^(m)-labeled glucose metabolism imaging agent,MAMA-conjugated azadibenzocyclooctyne derivative and four 2-azido glucose derivatives were synthesized.Two potential candidates(N_(3)-DG-1 and N_(3)-DG-2)were selected according to the in vitro kinetic study experiment.The 2-azido glucose derivatives were pretargeted in mice bearing S180 tumor,then^(99)Tc^(m)-labeled MAMA-azadibenzocyclooctyne derivative was administrated to accomplish the in vivo copper-free click reaction and imaging of glucose metabolism.The biodistribution results showed that the tumor/blood and tumor/muscle ratios of N_(3)-DG-2 were higher than those of N_(3)-DG-1,indicating the combination of^(99)Tc^(m)-labeled MAMA-azadibenzocyclooctyne derivative and N_(3)-DG-2 was more suitable for glucose metabolism imaging.

关 键 词：葡萄糖代谢 体内无铜点击 肿瘤 锝-99m 放射性标记 

分 类 号：TL923[核科学技术—核燃料循环与材料] R817.9[医药卫生—影像医学与核医学]