^(99m)TcN-IPDTC的制备、生物分布及与^(99m)Tc-IPDTC的对比研究  

A STUDY ON PREPARATION AND BIODISTRIBUTION OF ^(99m)TcN-IPDTC AS A NEW BRAIN PERFUSION IMAGING AGENT AND COMPARISON WITH ^(99m)Tc-IPDTC

作　　者：张俊波[1] 王学斌[1] 

机构地区：[1]北京师范大学化学系,北京100875

出　　处：《北京师范大学学报（自然科学版）》2000年第5期670-673,共4页Journal of Beijing Normal University(Natural Science)

基　　金：北京市科委重点资助项目!(95 330 430 0 )

摘　　要：采用SnCl2 ·2H2 O为还原剂 ,丁二酰二酰肼 (SDH)为N3- 离子提供体 ,在室温下制备[99mTcN]2 + int 中间体 ,然后与配体二水·N 异丙基 二硫代氨基甲酸钠 (IPDTC)发生交换反应 ,得到放化纯度大于 90 %的99mTcN IPDTC配合物 .小鼠体内生物分布表明 ,99mTcN IPDTC有较高的脑摄取和较好的脑滞留 ,有望成为一类新型脑灌注显像剂 .为了对比99mTcN IPDTC与99mTc IPDTC的异同 ,同时采用甲脒亚磺酸 (FSA)作还原剂对配体IPDTC进行了99mTc直接标记 .小鼠生物分布结果表明 ,99mTc IPDTC主要在肝内浓集 ,而脑摄取很少 ,这也充分表明放射性药物分子中引入[99mTcN]2 + 核会引起生物分布性质的明显改变 .这些结果对于设计新型放射性药物具有重要参考价值 .m TcN IPDTC(IPDTC:N isopropyl dithiocarbamate dihydrate) is prepared through a two step ligand exchange reaction by using SnCl 2 ·2H 2 O as reduction agent and SDH (succinic dihydrazide) as a donor of nitride nitrogen atom (N 3- ) at room temperature. The radiochemical purity (RCP) of the product is over 90% by TLC. The biodistribution results in mice indicate that 99m TcN IPDTC has good brain uptake and retention, suggesting that it will be a new potential brain perfusion imaging agent. The ligand IPDTC is also labelled with 99m TcO - 4 directly by using FSA(Formamidine sulfinic acid) as reduction agent. The biodistribution results in mice suggest that 99m Tc IPDTC is mostly accumulated in liver whereas the brain uptake is very low. This fact proves that the introduction of the \[ 99m Tc≡N\] 2+ core into the molecular structure of a radiopharmaceutical may obviously alter its biological behavior. This study may be valuable for the design of a new radiopharmaceutical for clinical use.

关 键 词：^99MTC 锝氨核 放射性药物 脑摄取 生物分布 

分 类 号：TQ463.7[化学工程—制药化工]