~(99m)TcN(NOET)_2的标记、生物分布及与~(99m)Tc-NOET的对比研究

采用三（间－磺基苯基）膦（TPPS）作还原剂制备而得99mTcN（NOET）2（NOET：N－乙氧基，N－乙基氨荒酸钠），经TLC检测标记物的放化纳大于90％．将99mTcN（NOET）2进行了大鼠体内生物分布测试，结果表明99mTcN（NOET）2心肌摄取快而且摄取率高，5min心肌摄取量XID（即每克组织中含量占总注射量的百分比）为5．22％g-1，心肌滞留时间长，60min为3．09％g-1，有望进一步进行临床研究，同时采用甲脒亚磺酸（FSA）作还原剂对NOET进行了99mTc直接标记，大鼠生物分布结果表明99mTc－NOET主要在肝内浓集，而心肌摄取很少，这也充分表明，放射性药物分于中［99mTcN］2＋核结构的变化引起生物分布性质的明显改变．

A STUDY ON ~(99m)TcN(NOET)_2 LABELLING,BIODISTRIBUTION AND COMPARISON BETWEEN ~(99m)TcN(NOET)_2 AND ~(99m)Tc-NOET

99mTcN(NOET)2 is prepared by using TIPS as reduction agents. The radiochemical purity (RCP) of the product is over 90% by TLC. The biodistribution results in rats indicate 99mTcN(NOET)2 has good myocardial uptake and retention, and it will be used in clinical research. The ligand NOET is also labelled with 99mTcO4, directly by using FSA (Formamidine sulfinic acid) as reduction agent. The biodistribution results in rats suggest 99mTc-NOET is mostly accumulated in liver, whereas the myocardial uptake is very low. This fact proves that the introduction of the 99mTc=N]2+ core into the molecular structure of a radiopharmaceutical may obviously alter its biological behavior.