为快速、高效合成中枢神经阿片受体显像剂11 C-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,11 C-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-[(l-oxopropyl) phenylamino]-l-(2-phenylethyl) , sodium salt as precursor in DMSO solution. The radio-chemical 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.
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