^99Tc^m(CO)3^＋核心标记的邻二氮杂菲类化合物的理化性质和生物分布  

Preparation and Evaluation of New [^(99)Tc^m(CO)_3]^+-Labelled Phenanthroline Complexes

作　　者：杨洋[1] 韩美娇[1] 王科志[1] 朱霖[1] 

机构地区：[1]育部放射性药物重点实验室,北京师范大学化学学院,北京100875

出　　处：《核化学与放射化学》2009年第3期152-156,共5页Journal of Nuclear and Radiochemistry

基　　金：国家“973”项目(2006CB500705);国家自然科学基金资助项目(20371008,90401007)

摘　　要：确定化合物可以通过血脑屏障进入脑中并迅速从脑中清除,是判断药物能否作为阿尔茨海默病显像剂的首要条件。为发展99Tcm标记的阿尔茨海默病早期显像诊断药物,在前期研究与DNA分子结合的荧光探针钌金属配合物的基础上,设计合成了2个邻二氮杂菲类配体2-(9-蒽基)-1氢-咪唑[4,5-f][1,10]邻菲咯啉(2-(9-anthryl)-1H-imidazo[4,5-f][1,10]phenanthroline,aip)和2-(9-蒽基)-1乙基-咪唑[4,5-f][1,10]邻菲咯啉(2-(9-anthryl)-1ethyl-imidazo[4,5-f][1,10]phenanthroline,aeip),并与99Tcm(CO)3+进行标记。采用R-HPLC、纸电泳等方法研究标记产物的理化性质。正常小鼠体内生物分布研究表明,2种化合物99Tcm(CO)3+-aip和99Tcm(CO)3+-aeip均有一定的脑初始摄取,注射后2min,前者为(1.028±0.096)%ID/g;后者为(1.191±0.197)%ID/g,因此标记物具有进一步研究的价值。The chief requirement to determine if pharmaceuticals may be AD-tracer is that complexes can pass through BBB to enter the brain and have rapid clean from the brain.To develop early diagnose radiopharmaceuticals for Alzheimer s disease,new phenanthroline complexes 2-（9-anthryl）-1H-imidazo[4,5-f][1,10]phenanthroline（aip） and 2-（9-anthryl）-1ethyl-imidazo[4,5-f][1,10]phenanthroline（aeip） based on the early research of Ru complexes banding to DNA used for fluescence method were synthesized and labelled by 99Tcm -tricarbonyl core. Radiochemical purities of complexes 99 Tcm （CO）＋-aip and 99 Tcm （CO）＋-aeip were found to be more than 95 % as proved by radio-HPLC. Paper electrophoresis show that these complexes are neutral. Biodistribution of these complexes in mice shows the higher early uptakes in brain （2 min, 99Tcm（CO）＋-aip： （1. 028±0. 096）%ID/g; 99Tcm（CO）3＋-aeip： （1. 191＋0. 197）%ID/g）.

关 键 词：阿尔茨海默病 羰基锝 邻二氮杂菲 脑摄取 

分 类 号：R817[医药卫生—影像医学与核医学]