新的异腈类配合物^(99m)TcN-CHI的制备与生物分布研究  

THE PREPARATION AND BIODISTRIBUTION OF A NEW TECHNETIUM-99m NITRIDO COMPLEX ^(99m) TcN-CYCLOHEXYLISONITRILE

作　　者：张现忠[1] 王学斌[1] 周金明[1] 

机构地区：[1]北京师范大学化学系,北京100875

出　　处：《北京师范大学学报（自然科学版）》2001年第5期671-674,共4页Journal of Beijing Normal University(Natural Science)

基　　金：北京师范大学青年科学基金 (理科 )资助项目 ( 10 7195 )

摘　　要：通过甲酰胺化和脱水 2步反应合成了配体环己基异腈 (CHI) ,对其进行了熔、沸点测定 ,红外和元素分析等表征。并以氯化亚锡为还原剂、二硫代肼基甲酸甲酯为供氮体 ,经配体交换反应制备了放化纯度大于 95 %的配合物99mTcN CHI .该配合物为脂溶性的 ,在室温下放置 6h以上放化纯度无明显变化 .在正常昆明小鼠体内进行的生物分布实验结果表明 ,99mTcN CHI在心肌中有一定摄取 ,但肝、肺、血等本底摄取相对较高 .动物实验结果还显示 ,该配合物在血液中有较高的浓集 ,其在静注后 5min时的血 /心、血 /肝和血 /肺单位质量组织摄取率的比值分别为 0 95 ,3 15和 1 33.有望通过对异腈配体结构的修饰而获得制备方法简单、生物性能优良的99mTc标记心血池显像剂 .An isonitrile ligand cyclohexylisonitrile (CHI) was synthesized and a copper salt [Cu(Ⅰ)(CHI) 4 BF 4 ] of this ligand was also prepared. The isonitrile and it's copper salt were characterized by IR and elemental analysis. The complex 99m TcN-CHI was prepared by ligand exchange reaction and the RCP of it was evaluated by TLC chromatography and ranged between 95%～98%. The result of stability study indicates that the complex is stable over a period of 6 h at room temperature. The complex 99m TcN-CHI shows high liver and blood uptake and has a certain heart uptake in mice. Compared with 99m Tc-CHI, the heart and lungs uptake of 99m TcN-CHI is less than that of 99m Tc-CHI significantly. Because of 99m TcN- CHI shows high blood uptake and low lungs, heart and liver uptake, thus it maybe suitable for cardiac blood pool imaging and further studies about it will be carried on.

关 键 词：^99mTcN核 环己基异腈 放射性药物 生物分布 心血池显像剂 异腈配合物 

分 类 号：O615.4[理学—无机化学] R981[理学—化学]