^(99)Tc^mN-TMCHI与^(99)Tc^m-TMCHI的制备与性质比较  

Preparation and Properties Comparison of ^(99)Tc^mN-TMCHI and ^(99)Tc^m-TMCHI

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：《同位素》2001年第3期140-144,共5页Journal of Isotopes

基　　金：北京师范大学青年科学基金 (理科 )资助项目 (1 0 71 95 )

摘　　要：以 3,3,5 -三甲基环己胺为原料 ,通过甲酰胺化和脱水两步反应制得配体 3,3,5 -三甲基环己基异腈 (TMCHI) ;并以氯化亚锡为还原剂、二硫代肼基甲酸甲酯为供氮体 ,通过配体交换反应得到放化纯度大于 95 %的 99Tcm N- TMCHI标记物。99Tcm- TMCHI配合物是以氯化亚锡为还原剂直接标记制得。两种标记物在室温下放置 6 h以上放化纯度均无明显变化。正常昆明小鼠体内的生物分布实验研究结果显示 :99Tcm N- TMCHI和 99Tcm- TMCHI在心、脑中有一定摄取 ,但肝、肺、血等本底摄取相对较高 ;二者在血液中都有很高的浓集 ,且滞留也很好 ,其中 99Tcm- TMCHI配合物在静注后 6 0min时的血与心、血与肝和血与肺摄取比分别为 6 .2 2、2 .16和 1.5 0。因此 ,有望通过对异腈配体结构的修饰 ,改变配合物的性能 ,从而获得制备方法简单、生物性能优良的An isonitrile ligand 3,3,5 trimethyl cyclohexylisonitrile(TMCHI) is synthesized and a copper salt (Cu(I)(TMCHI) 4BF 4) of this ligand is also prepared, the isonitrile and it's copper salt are characterized by IR and elemental analysis. The complex 99 Tc mN TMCHI is prepared by ligand exchange reaction and 99 Tc m TMCHI is prepared by 99 Tc m labelling directily with SnCl 2·2H 2O as reducing agent. The radiochemical purity of the two complexes are more than 95%. The results of stability study indicate that the two complexes are stable over a period of 6 h at room temperature. Biodistribution of the two complexes in mice indicate that they have a certain extent uptakes in myocardium and brain and retain in them for a certain time, but also they are mainly accumulated in blood and maintain in it very good. The T/NT ratios of the two complexes in mice are excellent as cardiac blood pool imaging agents. Based on these promising properties, they maybe suitable for cardiac blood pool imaging and the studies about it will be go on.

关 键 词：^99TC^M 心血池显像剂 TMCHI ^99Tc^mN-TMCHI ^99Tc^m-TMCHI 生物分布 锝99 心脏功能 放射性核素 标记物 

分 类 号：R816.2[医药卫生—放射医学] R817.9[医药卫生—临床医学]