^(99)Tc^m标记的邻甲硫基-N-β-巯基乙酰苯胺和硫醇混配复合物的制备及生物分布研究  

Preparation and biodistribution of ^(99)Tc^m mixed ligand complexes containing a tridentate N-(o-methylthiophenyl)-β-mercaptoacetamide and monodentate thiols

作　　者：段新红[1] 吕恭序[2] 王学斌[2] 

机构地区：[1]北京林业大学基础科学与技术学院,北京100083 [2]北京师范大学化学系,北京100875

出　　处：《核技术》2003年第11期863-867,共5页Nuclear Techniques

摘　　要：合成了新的三配位体邻甲硫基-N-β-巯基乙酰苯胺(MTPMA),其结构经红外光谱(IR)、核磁共振(HNMR)、质谱(Ms(FAB+))和元素分析确认。用配体交换方法制备了两种混合配位体复合物99Tcm(L3,L1a)和99Tcm(L3,L1b)。其中,L3为三配位体,L1a、L1b分别为单配位体乙硫醇和异丙硫醇。确定了这两种混配复合物的最佳标记条件,在此条件下,放射化学纯度(RCP)>90％,并且在室温下稳定6 h以上。99Tcm(L3,L1a)和99Tcm(L3,L1b)的小鼠生物分布研究表明:两种混配复合物都可通过正常的血脑屏障,并在脑中有一定滞留。A novel compond, N-(o-methylthiophenyl)-β-mercaptoacetamide (MTPMA),as a tridentate ligand,was synthesized and characterized by IR, 1HNMR, MS(FAB+) and elemental analysis. Two 99Tcm mixed-ligand complexes of 99Tcm (L3,L1a) and 99Tcm (L3,L1b) were produced by ligand exchange reaction. At the same time, the optimized conditions for labelling were obtained. At these conditions, the radiochemical purity of both complexes was better than 90% and they were stable over 6 h at room temperature. Biodistribution study showed that both complexes can penetrate the blood-brain barrier and exhibit retention in mice's brain .

关 键 词：混合配位体复合物 生物分布 血脑屏障 

分 类 号：O615.712[理学—无机化学] R817.9[理学—化学]