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    99Tcm (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 99Tcm (CO)3+-Labelled Phenanthroline Complexes

      摘要
    • 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-f1, 10邻菲咯啉（2-(9-anthryl)-1H-imidazo4, 5-f1, 10phenanthroline， aip)和2-(9-蒽基)-1乙基-咪唑4, 5-f1, 10邻菲咯啉(2-(9-anthryl)-1ethyl-imidazo4, 5-f1, 10phenanthroline， 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2 min，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。

       

      Abstract: 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-imidazo4, 5-f1, 10phenanthroline (aip) and 2-(9-anthryl)-1ethyl-imidazo4, 5-f1, 10phenanthroline (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 99Tcm (CO)+3-aip and 99Tcm-(CO)+3-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)+3-aip: （1.028±0.096）％ID/g; 99Tcm (CO)+3-aeip: （1.191±0.197）％ID/g).

       

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