Preparation and preliminary biological evaluation of ^(99m)Tc-ANMdU  

作　　者：LU Chunxiong JIANG Quanfu YU Huixin WANG Songpei Li Xiaomin WANG Zhengwu 

机构地区：[1]School of Chemical ＆ Material Engineering, Jiangnan University, Wuxi 214122, China [2]Key Laboratory of Nuclear Medicine, Ministry of Health/Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China [3]Department of Food Science ＆ Technology, School of Agriculture and Biology, Shanghai Jiao Tong University, Shanghai 200240, China

出　　处：《Nuclear Science and Techniques》2010年第2期106-109,共4页核技术（英文）

基　　金：Supported by National Natural Science Foundation of China (20573048 and 20676051);Natural Science Foundation of Jiangsu Province (BK2008111, BK2008112);Department of Health of Jiangsu Province (H200624)

摘　　要：Technetium-99m-labeled-5-{2-sulfanylethyl-[2-(2-sulfanylethylamino)acetyl]amino}-methyl-2′-deoxy- uridine (99mTc-ANMdU) was reported. The precursor ANMdU was synthesized by six-step reactions and all intermediates were verified with MS and 1HNMR. Using SnCl2 as reducing agent, a labeling reaction was carried out at 100°C for 30 min. The radiochemical purity of the 99mTc-ANMdU was 96.68%. Partition coefficients were 0.92 and 0.70 at pH 7.0 and 7.4 of the phosphate buffer saline, respectively. Biodistribution of 99mTc-ANMdU in normal mice showed that the initial uptake of 99mTc-ANMdU in vivo and the clearance was rapid.Technetium-^99m-labeled-5- {2-sulfanylethyl- [2-（2-sulfanylethylamino）acetyl]amino }-methyl-2＇-deoxy- uridine （^99mTc-ANMdU） was reported. The precursor ANMdU was synthesized by six-step reactions and all intermediates were verified with MS and 1HNMR. Using SnCl2 as reducing agent, a labeling reaction was carried out at 100℃ for 30 min. The radiochemical purity of the ^99mTc-ANMdU was 96.68%. Partition coefficients were 0.92 and 0.70 at pH 7.0 and 7.4 of the phosphate buffer saline, respectively. Biodistribution of ^99mTc-ANMdU in normal mice showed that the initial uptake of ^99mTc-ANMdU in vivo and the clearance was rapid.

关 键 词：生物制备 放射化学纯度 评价 磷酸盐缓冲液 1HNMR 氯化亚锡 分配系数 中间体 

分 类 号：TQ457.2[化学工程—农药化工] TS245.9[轻工技术与工程—制糖工程]