^(99)Tc^m标记的N-(邻甲硫基苯基)乙二胺和硫醇混配配合物的制备及生物分布

SYNTHESIS AND BIODISTRIBUTION OF ^(99)Tc^m MIXED LIGAND COMPLEXES CONTAINING A TRIDENTATE N-(O-METHYLTHIOPHENYL)ETHYLENEDIAMINE AND MONODENTATE THIOLS

合成了新的三齿配体N (邻甲硫基苯基)乙二胺(MTPEA),并经IR、元素分析、MS(FAB+)表征确认。确定了混配配合物99Tcm(L3,L1a)(L3为MTPEA,L1a为乙硫醇)和99Tcm(L3,L1b)(L1b为异丙硫醇)的最佳标记条件。标记物在小鼠体内的生物分布结果表明:这两种配合物都可以通过正常的血脑屏障,并在脑中有一定的滞留。在注射后2,30min,99Tcm(L3,L1a)的脑摄取值分别为2.09%/g和1.10%/g;99Tcm(L3,L1b)的脑摄取值分别为1.76%/g和1.08%/g。

A new ligand N(OMethylthiophenyl)ethylenediamine(MTPEA) is synthesized and characterized by IR, MS(FAB+) and elemental analysis. The preparation of two 99Tcmmixedligand complexes is studied by ligand exchange reaction. At the same time, the optimal conditions for labelling are obtained. The biodistribution study shows that both complexes could thread the bloodbrain barrier and in brain for a certain time.