^(99m)Tc标记COI配合物的制备及其用作心室显像剂的初步研究  

Preparation and Biodistribution of a Novel Potential Blood Pool Imaging Agent Technetium-99m Labeled COI Complexes

作　　者：张现忠[1] 周金明[1] 王学斌[1] 

机构地区：[1]北京师范大学化学系,北京100875

出　　处：《高等学校化学学报》2002年第10期1829-1832,共4页Chemical Journal of Chinese Universities

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

摘　　要：通过改变异腈配体的结构和配合物的中心核 ,以期获得标记方法简单、放化纯度高以及生物性能优良的新型心室显像剂 .以环辛胺为原料 ,通过甲酰胺化和脱水两步反应制得配体环辛基异腈 (COI) ,并以氯化亚锡为还原剂和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 99m Tc N-COI标记物 .以氯化亚锡为还原剂直接标记制得放化纯度大于 95 %的99m Tc-COI配合物 .两种标记物在室温下放置 6h以上 ,其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研究结果显示 ,99m Tc N-COI和 99m Tc-COI在心脑中有一定摄取 ,但肝、肺及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 99m Tc-COI配合物在静脉注射后 60 min时的血 /心、血 /肝和血 /肺摄取比分别为 6.67,1 .5 4和 2 .0 7。The objective of this study is to develop a new potential cardiac blood pool imaging agent. An isonitrile ligand cyclooctylisonitrile(COI) is synthesized and a copper salt[Cu(Ⅰ)(COI) 4BF 4] of this ligand is also prepared, the isonitrile and it′s copper salt are characterized by IR and elemental analysis. The complex 99mTcN-COI is prepared by ligand exchange reaction while the complex 99mTc-COI is prepared by a direct labeling method. The results of stability study indicated that both complexes are stable over a period of 6 h at room temperature. The biodistribution of these new complexes in mice indicated that they had significantly different uptake properties in most tissues. But they are all mainly accumulated in blood and maintained in it very good. Especially the T/NT ratios of 99mTc-COI in mice are excellent as a cardiac blood pool imaging agent. Based on its promising properties, the complex 99mTc-COI maybe suitable for cardiac blood pool imaging.

关 键 词：标记 COI配合物 制备 心室显像剂 ^99Tc-COI 体内生物分布 锝99 环辛基异腈 放射性标记药物 

分 类 号：R817.4[医药卫生—影像医学与核医学]