【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.更多还原

【Abstract】 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 99mTc 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.更多还原