| 99Tcm标记基于体内无铜点击化学的葡萄糖代谢显像剂 |
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| 引用本文： | 陈庆鑫,褚泰伟.99Tcm标记基于体内无铜点击化学的葡萄糖代谢显像剂[J].同位素,2021,34(4):346. |
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| 作者姓名： | 陈庆鑫 褚泰伟 |
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| 作者单位： | 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 |
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| 摘 要： | 为了发展99Tcm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（N3-DG-1和N3-DG-2）。首先完成N3-DG-1和N3-DG-2在荷S180肿瘤小鼠体内的预着靶，再注射99Tcm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，N3-DG-2的瘤血比和瘤肉比优于N3-DG-1，说明99Tcm标记的环辛炔探针和N3-DG-2组合更适用于葡萄糖代谢显像。
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| 关 键 词： | 葡萄糖代谢 体内无铜点击 肿瘤 锝-99m 放射性标记 |
99Tcm-labeled Glucose Metabolism Imaging Agents Based on in Vivo Copper-free Click Chemistry |
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| CHEN Qingxin,CHU Taiwei.99Tcm-labeled Glucose Metabolism Imaging Agents Based on in Vivo Copper-free Click Chemistry[J].Isotopes,2021,34(4):346. |
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| Authors: | CHEN Qingxin CHU Taiwei |
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| Affiliation: | Radiochemistry and Radiation Chemistry Key Laboratory of Fundamental Science, College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China |
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| Abstract: | In order to develop an ideal 99Tcm-labeled glucose metabolism imaging agent, MAMA-conjugated azadibenzocyclooctyne derivative and four 2-azido glucose derivatives were synthesized. Two potential candidates (N3-DG-1 and N3-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 99Tcm-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 N3-DG-2 were higher than those of N3-DG-1, indicating the combination of 99Tcm-labeled MAMA-azadibenzocyclooctyne derivative and N3-DG-2 was more suitable for glucose metabolism imaging. |
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| Keywords: | glucose imaging in vivo copper-free click chemistry tumor technetium-99m radio labeling |
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