~(99)Tc~m-MPAQ的合成及其生物分布
SYNTHESIS AND BIODISTRIBUTION OF ~(99) Tc~m-MPAQ
-
摘要: 为寻找新的99Tcm脑灌注显像剂,对99Tcm MPBDA进行了结构修饰。在制备N (2 巯基丙基) 1,2 苯二胺(MPBDA)基础上合成了三齿配体8 N (2 巯基丙基) 氨基喹啉(MPAQ),产物经IR,1HNMR,MS及元素分析等表征确认。以氯离子为单齿配体,用直接标记法制备了99Tcm MPAQ,确定了最佳标记条件,测定了标记物的稳定性和脂溶性。实验结果表明,99Tcm MPAQ放化纯在96%以上,室温下在水溶液中稳定6h以上,脂溶性比99Tcm MPBDA的大。生物分布试验结果表明,99Tcm MPAQ生物性质没有99Tcm MPBDA的好,但它可以穿过正常的血脑屏障,有一定的脑摄取(1.55%/g)和脑滞留(注射后30min仍有初始摄入量的62%)。Abstract: In order to find new Tc-99m complexes for brain per fusion agent, modification of 99 Tc m-MPBDA structure is performed. Tridentate ligand MPAQ is synthesized based on preparation of MPBDA. The products have been characterized by IR, 1H NMR, MS and element analysis. Preparation of “3+1” mixed-ligand complex 99 Tc m-MPAQ is carried out with direct reduction by using Cl -as monodentate ligand. The labeling conditions are optimized. The lipophilicity and stability of 99 Tc m-MPAQ are tested. The results demonstrate that radiochemical purity of 99 Tc m-MPAQ is over 96% with a high stability in aqueous solution and a higher lipophilicity than that of 99 Tc m-MPBDA. Biodistribuion study in ICR mice indicates that although 99 Tc m-MPAQ is no better than 99 Tc m-MPBDA in biological properties, it can cross intact blood brain barrier(1.55 %/g at 5 min post injection) and retain for a certain time(62% remains in brain at 30 min post injection).
下载: