~(99)Tc~mN-CHDTC的制备,生物分布及与~(99)Tc~m-CHDTC的对比

    PREPARATION AND BIODISTRIBUTION OF ~(99)Tc~mN-CHDTC AND COMPARISON WITH ~(99) Tc~m-CHDTC

    • 摘要: 以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99TcmN2 +int 中间体 ,然后与二水·N 环己基 二硫代氨基甲酸钠 (CHDTC)发生配位体交换反应得到放化纯大于 90 %的99TcmN CHDTC配合物。小鼠体内的生物分布实验表明 ,99TcmN CHDTC有较高的脑摄取和较好的脑滞留。注射后 5,30 ,6 0min时 ,脑摄取量 (% /g)分别为 2 91,5 88,5 91,R(脑 /血 )比值分别为 0 14,1 4 6 ,2 10。99TcmN CHDTC在心肌中也有较高的摄取 ,但R(心 /肝 )比值低。采用甲脒亚磺酸 (FSA)作还原剂对配位体CHDTC进行99Tcm 直接标记 ,其在小鼠体内的生物分布结果表明 ,99Tcm CHDTC主要蓄积在肝脏 ,脑、心肌摄取很少。这表明放射性药物分子中引入 99TcmN2 +核会引起生物分布性质的明显改变

       

      Abstract: Tc mN CHDTC(CHDTC:N cyclohexyl dithiocarbamate dihydrate) is 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 radiochemical purity (RCP) of the product is over 90% by TLC. The biodistribution results in mice indicate that 99 Tc mN CHDTC has good brain uptake and retention, suggesting that it will be a new potential brain perfusion imaging agent. 99 Tc mN CHDTC also exhibits high myocardial uptake, but the R (heart/liver) is low thereby restricting the use of the complex as a good myocardial perfusion imaging agent. The ligand CHDTC is also labelled with 99 Tc mO 4 - directly by using FSA (formamidine sulfinic acid) as reduction agent. The biodistribution results in mice suggest 99 Tc m CHDTC is mostly accumulated in liver, whereas the heart and brain uptake is very low. This fact proves that the introduction of the 99 Tc m≡N 2+ core into the molecular structure of a radiopharmaceutical may obviously alter its biological behavior.

       

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