乙酰胆碱酯酶活性的PET显像剂-[^(11)C]MP4A的制备  

The Preparation of [~11c] MP4A, a PET Imaging Agent for Brain Acetylcholinesterase Activity

作　　者：周玲[1] 胡名扬 管一晖[3] 薛方平[3] 张政伟[3] 刘平[3] 丁正同[1] 蒋雨平[1] 

机构地区：[1]复旦大学上海医学院神经病学系 [2]上海医学生命科学研究中心有限公司,200032 [3]复旦大学附属华山医院PET中心,200040

出　　处：《中国临床神经科学》2008年第4期346-351,共6页Chinese Journal of Clinical Neurosciences

基　　金：上海市经济委员会资助课题(编号:05JYYY-49);项目负责人:蒋雨平

摘　　要：目的:合成能反映脑乙酰胆碱酯酶活性的PET显像剂[^(11)C]4-乙酰氧基-N-甲基哌啶([^(11)C]MP4A)的前体4-乙酰氧基哌啶(P4A),制备[^(11)C]MP4A。方法:合成MP4A前体P4A,利用[^(11)C]碘代甲烷合成模块合成的[^(11)C]碘代甲烷([^(11)C] CH_3I)直接与P4A反应制备[^(11)C]MP4A,或将[^(11)C]CH_3I通过三氟甲基磺酸银柱转化为[^(11)C]-三氟甲基磺酸甲酯([^(11)C]- Triflate-CH_3)后再与P4A反应制备[^(11)C]MP4A。结果:P4A化学纯度达99%以上。采用[^(11)C]-Triflate-CH_3制备的[^(11)C] MP4A放化纯>98%,轰击结束后(EOB)放射合成时间为20min,校正衰变后产率为40%～55%。结论:采用[^(11)C]-Triflate- CH_3制备的[^(11)C]MP4A放化纯度高,产率高。To synthesize of the precursor 4-piperidyl acetate for the production of N-[^11C]methyl-4-piperidyl acetate （[^11C]MP4A）, a tracer for measurement brain acetylcholinesterase （ACHE） level by using positron emission tomography （PET）. To set up the method of radiolabeling [HC]MP4A. Methods： Synthesize the precursor P4A[^11C]methyl iodide synthesized by using [^11C] methyl iodide automatic synthesis module, was reacted with P4A directly or reacted with P4A after converted to [^11C]-Triflate-CH3 to form [^11C]MP4A. Results： The chemical purity of precursor synthesized by using our method was 〉99%. The radiochemical purity of [^11C]MP4A was produced with 〉98% by means of [HC]-Triflate-CH3 and with 20 min of synthesis time after EOB, with yields ranging 40%-55% （decay-corrected）. Conclusion： The chemical purity and the yield of [^11C]MP4A prepared by using our precursor was high enough to be used in the further study.

关 键 词：乙酰胆碱酯酶 正电子发射断层扫描 制备 [^11C]4-乙酰氧基-N-甲基哌啶 

分 类 号：R742.5[医药卫生—神经病学与精神病学] R817.4[医药卫生—临床医学]