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| 乙酰胆碱酯酶活性的PET显像剂-[^11C]MP4A的制备 | |
| 引用本文： | 周玲,胡名扬,管一晖,薛方平,张政伟,刘平,丁正同,蒋雨平. 乙酰胆碱酯酶活性的PET显像剂-[^11C]MP4A的制备[J]. 中国临床神经科学, 2008, 16(4): 346-351 |
| 作者姓名： | 周玲 胡名扬 管一晖 薛方平 张政伟 刘平 丁正同 蒋雨平 |
| 作者单位： | 1. 复旦大学上海医学院神经病学系、复旦大学附属华山医院神经内科 200040 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 |
| 基金项目： | 上海市经济委员会资助课题 |
| 摘 要： | 目的：合成能反映脑乙酰胆碱酯酶活性的PET显像剂[^11C]4-乙酰氧基-N-甲基哌啶（[^11C]MP4A）的前体4-乙酰氧基哌啶（P4A），制备[^11C]MP4A。方法：合成MP4A前体P4A，利用[^11C]碘代甲烷合成模块合成的[^11C]碘代甲烷（[^11C]CH3I）直接与P4A反应制备[^11C]MP4A，或将[^11C]CH3I通过三氟甲基磺酸银柱转化为[^11C]-三氟甲基磺酸甲酯（[^11C]-Triflate-CH3）后再与P4A反应制备[^11C]MP4A。结果：P4A化学纯度达99％以上。采用[^11C]-Triflate-CH3制备的[^11C]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[^11C]-Triflate-CH3制备的[^11C]MP4A放化纯度高，产率高。 |
| 关 键 词： | 乙酰胆碱酯酶 正电子发射断层扫描 制备 4-乙酰氧基-N-甲基哌啶 |
The Preparation of[11C]MP4A,a PET Imaging Agent for Brain Acetylcholinesterase Activity |
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| ZHOU Ling HU Ming-Yang GUAN Yi-Hui XUE Fang-Ping ZHANG Zheng-Wei LIU Ping DING Zheng Tong JIANG Yu-Ping. The Preparation of[11C]MP4A,a PET Imaging Agent for Brain Acetylcholinesterase Activity[J]. Chinese Journal of Clinical Neurosciences, 2008, 16(4): 346-351 | |
| Authors: | ZHOU Ling HU Ming-Yang GUAN Yi-Hui XUE Fang-Ping ZHANG Zheng-Wei LIU Ping DING Zheng Tong JIANG Yu-Ping |
| Affiliation: | ZHOU Ling HU Ming-Yang GUAN Yi-Hui XUE Fang-Ping ZHANG Zheng-Wei LIU Ping DING Zheng Tong JIANG Yu-Ping Department of Neurology,Shanghai Medical College,Huashan Hospital,Fudan University,Shanghai 200040, 2 Shanghai Med Co,Ltd.,Shanghai 200032 3 PET Center,Huashan Hospital,Fudan University,Shanghai 200040,China |
| Abstract: | Aim: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 [~11C]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-CH_3 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 [~11C]_Triflate_CH_3 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. |
| Keywords: | acetylcholinesterase positron emission tomography preparation N-[~11C]methyl-4-piperidyl acetate |
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