脑乙酰胆碱酯酶活性PET显像剂[^(11)C]4-乙酰氧基-N-甲基哌啶纯化及鉴定的研究  

Investigation of purification and identification on N-[^(11)C]Methylpiperidin-4-yl acetate as PET imaging agent of brain acetylcholinesterase activity

作　　者：毛洁萍[1] 丁正同[2] 朱秋毓[3] 吴平[4] 管一晖[4] 胡名扬 张政伟[4] 薛方平[4] 刘平[4] 杨新玲[1] 蒋雨平[2] 

机构地区：[1]新疆医科大学第一附属医院,乌鲁木齐830054 [2]复旦大学附属华山医院神经内科 [3]复旦大学附属华山医院肾病科 [4]复旦大学附属华山医院PET中心 [5]上海医学生命科学研究中心有限公司

出　　处：《临床神经病学杂志》2010年第3期206-208,共3页Journal of Clinical Neurology

基　　金：上海市引进技术的吸收与创新计划项目(编号:08-082);上海市科技基金重大基础课题(编号:07DJ14005)

摘　　要：目的研究脑乙酰胆碱酯酶(AChE)活性PET显像剂[11C]4-乙酰氧基-N-甲基哌啶(MP4A)的纯化及其鉴定方法。方法用半制备高效液相色谱(HPLC)法,用强极性半制备柱PlatinumEPSC-18分离纯化[11C]MP4A粗产品,流动相使用乙酸铵-乙醇二元体系,一步法收集[11C]MP4A。用UV串联电化学(ECD)法和同位素法检测鉴定终产物[11C]MP4A的化学纯度及放射性纯度。结果用此纯化方法 ,前体(P4A)的保留时间为(2.5±0.3)min;MP4A的保留时间为(9.0±0.3)min;MP4A与P4A及其他杂质完全分离。纯化后的[11C]MP4A终产物经ECD和同位素法检测鉴定,其化学纯度达99%以上,放射纯度达100%。结论用半制备HPLC法可获得高纯度的[11C]MP4A,用ECD和同位素法鉴定准确率高,且本纯化、鉴定方法耗时短,有助于提高[11C]MP4A的质量和产量。Objective To study the methods for the purification and identification of N-[11C]Methylpiperidin-4-yl acetate （MP4A） as PET imaging agent of brain acetylcholinesterase activity.Methods An extended polar semi-preparation column was applied to the separation and purification of radioactive crude [11C]MP4A. The mobile phase consisted simply of a binary mixture of ammonium acetate with ethanol. The purities in chemistry and in radiochemistry of [11C]MP4A after one-step purification were confirmed by a combination method of ultra-violet spectrophotometry in tandem with electrochemical detection（ECD） and isotopic determination,respectively.Results Using the improved method,the retention time of the precursor（P4A） and the [11C]MP4A were （2.0±0.3）min and （9.0±0.3）min,respectively. And the MP4A was completely separated from P4A and other impurities.The purity for collected fraction of [11C]MP4A was over 99% in chemistry and was 100% in radiochemistry,respectively.Conclusion The radio-labeling [11C]MP4A with high purity in both chemistry and radiochemistry can be harvested with the methods of ECD and isotopic determination. The accuracy of identification with the method in the present study is high,the time-consuming is less. Moreover,it is helpful to improve product quality and quantity.

关 键 词：乙酰胆碱酯酶活性 PET显像剂 [11C]4-乙酰氧基-N-甲基哌啶 

分 类 号：R817.9[医药卫生—影像医学与核医学]