| 两种新型99mTc配合物的制备和初步生物分布研究 |
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| 引用本文： | 王凤龙,王学斌,张现忠.两种新型99mTc配合物的制备和初步生物分布研究[J].北京师范大学学报(自然科学版),2009,45(2). |
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| 作者姓名： | 王凤龙 王学斌 张现忠 |
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| 作者单位： | 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,100875,北京 |
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| 基金项目： | 国家自然科学基金资助项目(20401004) |
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| 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.
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| 关 键 词： | 5-HT1A受体 1 4 8 11-四氮杂环十四烷 MPPC配体 WAY100635 |
PREPARATION AND BIOLOGICAL EVALUATION OF TWO NOVEL 99mTc-COMPLEXES |
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| WANG Fenglong,WANG Xuebin,ZHANG Xianzhong.PREPARATION AND BIOLOGICAL EVALUATION OF TWO NOVEL 99mTc-COMPLEXES[J].Journal of Beijing Normal University(Natural Science),2009,45(2). |
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| Authors: | WANG Fenglong WANG Xuebin ZHANG Xianzhong |
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| Institution: | Key Laboratory of Radiopharmaceuticals of Ministry of Education;College of Chemistry:Beijing Normal University;100875;Beijing;China |
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| 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 pharm... |
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| Keywords: | 5-HT1A receptor cyclam MPPC WAY 100635 |
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