两种新型^99mTc配合物的制备和初步生物分布研究  

PREPARATION AND BIOLOGICAL EVALUATION OF TWO NOVEL ^(99m)Tc-COMPLEXES

作　　者：王凤龙[1] 王学斌[1] 张现忠[1] 

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

出　　处：《北京师范大学学报（自然科学版）》2009年第2期172-175,共4页Journal of Beijing Normal University(Natural Science)

基　　金：国家自然科学基金资助项目(20401004)

摘　　要：为了制备适于99mTc标记的5-HT1A受体显像剂,将WAY100635中具有生物活性的1-(2-甲氧基苯基)哌嗪(MPP)部分与双功能联接剂1,4,8,11-四氮杂环十四烷(cyclam)相连接制得MPPC配体,再分别利用99mTcN核和99mTcO2核进行标记,得到新型电中性的99mTcN-MPPC和正电荷的99mTcO2-MPPC配合物,2种配合物经薄层色谱(TLC)和高效液相色谱(HPLC)鉴定,放射化学纯度都在95%以上.这提供了1种将99mTc连接到WAY100635药效基团的新方法.2种配合物均呈水溶性,并可在室温下稳定存在6h以上.小鼠生物分布结果表明:2种配合物在脑中均有一定的摄取和滞留,且99mTcN-MPPC的初始脑摄取明显高于99mTcO2-MPPC.To prepare 99mTc complexes as potential imaging agent for the 5-HT1A receptor, the 1-（2- methoxyphenyl）piperazine moiety of WAY 100635 was introduced into the structure of the cyclam and two novel 99rnTc complexes were obtained： the neutral 99mTcN-MPPC and the cationic 99mTcO2-MPPC, containing 99mTc（V）-nitrido and 99mTc（V）-dioxo cores, respectively. The complexes were analyzed by TLC and HPLC, the radiochemical purity was found to be above 95%. This paper provides a novel method for attaching technetium to the pharmacophore moiety of WAY 100635. These two complexes were hydrophilic and stable for at least 6 h at room temperature. Biodistribution study in mice demonstrated uptake in the brain, and 99mTcN-MPPC uptake was significantly higher than 99mTcO2-MPPC.

关 键 词：5-HT1A受体 1 4 8 11-四氮杂环十四烷 MPPC配体 WAY100635 

分 类 号：O641.4[理学—物理化学] TQ463.7[理学—化学]