~(99)Tc~m标记的N-(邻甲硫基苯基)甘氨酰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 COMPLEX CONTAINING A TRIDENTATE N(O-METHYLTHIOPHENGL) GLYCINAMIDE AND A MONODENTATE THIOL

摘要: 合成了三齿配位体N (邻甲硫基苯基 )甘氨酰胺 (MTPGA)。其结构经IR、NMR及MS等表征予以确认。用配位体交换法制备了99Tcm(L1,L3)混配配合物 (其中L1为单齿配位体乙硫醇 ,L3为三齿配位体MTPGA) ,确定了标记的最佳条件及标记物的稳定性。实验结果表明 ,99Tcm(L1,L3)的标记率在 90 %以上 ,室温下可以稳定约 6h。用99Tcm(L1,L3)进行了小鼠生物分布研究。结果表明 ,该配合物可以通过正常的血脑屏障 ,有一定的初始脑摄取。

Abstract: A new compound N (O methyl thiophenyl) glycinamide as a ligand is synthesized and charaterized by IR, 1H NMR and MS(FAB). Preparation of 99 Tc m mixed ligand is carried out by ligand exchange reaction. The labeling condition is optimized. Biodistribution of this new 99 Tc m mixed ligand complex in rats shows that it can pass through the blood brain barrier and retain for a certain time in brain.