~(99)Tc~mN-DMSA的制备及其生物分布

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 [99TcmN]2 + 中间体 ,然后与二巯丁二酸 (DMSA)发生配体交换反应 ,得到放射化学纯度大于 90 %的 99TcmN DMSA配合物。99TcmN DMSA在室温下 6h内稳定 ,脂水分配系数lgP =- 3.74 ,表明是一水溶性化合物。99TcmN DMSA在小鼠体内生物分布表明 ,与作为肾显像剂的99Tcm DMSA相比 ,其生物分布发生了较大的变化 ,99TcmN核的引入导致了较高的骨摄取值和较低的肾摄取值

Synthesis and Biodistribution of 99TcmN-DMSA Complex

The complex 99 Tc mN DMSA (DMSA:Dimercaptosuccinic acid) is synthesized through ligand exchange reaction.The two step procedure involves the initial reaction of 99 Tc mO 4 -with succinic dihydrazide(SDH) as a donor of nitride nitrogen atom (N 3- ) in the presence of stannous chloride dihydrate as reductive agent and propylenediamine tetraacetic acid(PDTA) as complexant,followed by addition of the DMSA ligand.The radiochemical purity (RCP) of the product is over 90% measured by thin layer chromatography (TLC).The conditions of preparation for the 99 Tc mN DMSA complex are optimized .The stability and the partition coefficient of the 99 Tc mN DMSA complex are studied.It is stable over 6 h at room temperature.Its partition coefficient(lg P =-3.74) indicates it is a good hydrophilic complex.The biodistribution results in mice indicate that the 99 Tc mN DMSA complex is accumulated in bone with high uptake and good retention and less kidney uptake,suggesting it will be potentially useful as the first bone imaging agent containing the [ 99 Tc mN] 2+ core.The biodistribution comparison in mice of the 99 Tc mN DMSA complex with the 99 Tc m DMSA complex indicates that the presence of the 99 Tc m nitrido group significantly alters the biological properties of the 99 Tc m complex.