胆碱模块自动化合成^(11)C-carfentanil及Micro PET显像  

Automated Synthesis of ^(11)C-carfentanil With ^(11)C-choline Module and Micro PET Imaging

作　　者：张锦明[1] 徐志红 张晓军[1] 向晓辉[3] 田嘉禾[1] 

机构地区：[1]中国人民解放军总医院核医学科,北京100853 [2]江常熟苏华益化工有限公司,江苏常熟215522 [3]北京大学神经科学研究所,北京100191

出　　处：《同位素》2011年第3期182-187,共6页Journal of Isotopes

基　　金：国家重点研究发展计划(973)资助项目(2007CB512500)

摘　　要：为快速、高效合成中枢神经阿片受体显像剂11C-carfentanil(11C-CFN),对国产商业化11C-胆碱合成模块略做改动,并优化了合成条件。结果表明,采用4-哌啶乙酸钠,4-[(1-丙羰基)苯胺]-1-(2-苯乙基)[钠盐]作前体,DMSO作溶剂,11CH3-triflate作甲基化试剂,在胆碱模块上采用反应瓶法,可自动化合成11C-CFN。合成的11C-CFN活度>14.8 GBq、比活度>1.4×1014Bq/g、放化纯度>99%,校正合成效率>80%(n=55,以11CH3-triflate计算),全部合成时间为18 min。经Micro PET/CT证实,11C-CFN可用于μ阿片受体的PET显像研究。A simple modified home-made 11C-choline module enabled to rapid and efficient synthesis 11C-carfenatnil（11C-CFN） as CNS μ-opioid receptor imaging agent.The synthesis of 11C-CFN was completed in a yield of 14.8 GBq within 18 min from 11C-CO2 on the choline module.The methylation took place from 4-piperidinecarboxylic acid,4-[（1-oxopropyl）phenylamino]-1-（2-phenylethyl）,sodium salt as precursor in DMSO solution.The radiochemical yields were over 80%（n=55,decay-corrected and based on 11CH3-triflate）.The radiochemical purity was over 95% and the specific activities was over 1.4×1014 Bq/g.The biologic activity of 11C-CFN was confirmed with Micro PET/CT imaging.

关 键 词：11C-carfentanil(11C-CFN) 胆碱模块 自动化合成 PET显像 

分 类 号：R817[医药卫生—影像医学与核医学]