^(99m)TcN-IBDTC与^(99m)Tc-IBDTC的对比研究  

A study of comparison between ^(99m)TcN-IBDTC and ^(99m)Tc-IBDTC

作　　者：张俊波[1] 王学斌[1] 

机构地区：[1]北京师范大学,北京100875

出　　处：《核技术》2001年第11期933-936,共4页Nuclear Techniques

摘　　要：为了检验配合物分子中 [99mTcN]2 + 中心核的引入对其生物分布的影响以求找到一种新的放射性药物。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N -异丁基 -二硫代氨基甲酸钠 (IBDTC)发生配体交换反应得到99mTcN -IBDTC配合物。同时采用甲脒亚磺酸 (FSA)作还原剂对配体IBDTC进行了99mTc直接标记。结果表明 ,99mTcN -IBDTC和99mTc -IBDTC配合物的放化纯均大于 90 % ,小鼠体内生物分布表明 ,99mTcN -IBDTC有较高的脑摄取和较好的脑滞留 ,在注射后 5、30、6 0min时脑摄取量 (%ID·g- 1)分别为 6 .2 2、5 .4 5、3.88,脑 /血比值分别为 1.5 1、2 .2 4、1.84 ,有望成为一类新型脑灌注显像剂。99mTcN -IBDTC在心肌中也有较高的摄取 ,但心肌清除快而且心 /肝比值低从而限制了其成为一类新型心肌灌注显像剂。99mTc -IBDTC主要在肝内浓集 ,而脑、心肌摄取很少。本实验提示 ,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 ,这对于设计新型放射性药物具有参考价值。The aim of this study is to examine the influence on biodistribution by introducing the [ 99m Tc≡N] 2+ core into the complex so as to explore a new radiopharmaceutical. 99m TcN-IBDTC (IBDTC:N-isobutyl dithiocarbamate) was prepared through a two-step ligand-exchange reaction by using SnCl 2·2H 2O as reduction agent and SDH (succinic dihydrazide) as a donor of nitride nitrogen atom (N 3- ) at room temperature. The ligand IBDTC was labelled with 99m TcO - 4 directly by using FSA (Formamidine sulfinic acid) as reducing agent. The radiochemical purity of the 99m TcN-IBDTC and 99m Tc-IBDTC complex were both over 90% by TLC. The biodistribution results in mice indicated that 99m TcN-IBDTC had high brain uptake and good brain retention. The brain uptake (%ID·g -1 ) was 6.22, 5.45 and 3.88 and the brain/blood ratios were 1.51, 2.24 and 1.84 at 5, 30 and 60min post-injection respectively. The results suggested that it would be potentially useful as a brain perfusion imaging agent. 99m TcN-IBDTC also exhibited high myocardial uptake, but the washout from the heart was rapid and the heart/liver ratio was low thereby restricting the use of the complex as a myocardial perfusion imaging agent. The biodistribution results in mice suggested 99m Tc-IBDTC was mostly accumulated in liver, whereas the brain and heart uptake was very low. This study 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 may be valuable for the design of new radiopharmaceuticals for clinical use.

关 键 词：^99mTcN-IBDTC ^99mTc-IBDTC 核医学放射性药物 生物分布 锝99 标记物 IBDTC 核医学 放射性核素 

分 类 号：R817.9[医药卫生—影像医学与核医学]