| 胆碱模块自动化合成11C-carfentanil及Micro PET显像 |
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| 引用本文： | 张锦明,徐志红,张晓军,向晓辉,田嘉禾.胆碱模块自动化合成11C-carfentanil及Micro PET显像[J].同位素,2011,23(3):182-187. |
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| 作者姓名： | 张锦明 徐志红 张晓军 向晓辉 田嘉禾 |
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| 作者单位： | 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 |
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| 基金项目： | 国家重点研究发展计划(973)资助项目(2007CB512500) |
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| 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。
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| 关 键 词： | 11C-carfentanil(11C-CFN) 胆碱模块 自动化合成 PET显像 |
Automated Synthesis of ~(11)C-carfentanil With ~(11)C-choline Module and Micro PET Imaging |
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| ZHANG Jin-ming,XU Zhi-hong,ZHANG Xiao-jun,XIANG Xiao-hui,TIAN Jia-he.Automated Synthesis of ~(11)C-carfentanil With ~(11)C-choline Module and Micro PET Imaging[J].Isotopes,2011,23(3):182-187. |
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| Authors: | ZHANG Jin-ming XU Zhi-hong ZHANG Xiao-jun XIANG Xiao-hui TIAN Jia-he |
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| Affiliation: | 1. Department of Nuclear Medicine, The PLA General Hospital, Beijing 100853, China;2. Isotopes Co, Jiangsu China， Changshu 215522, China;3. Neuroscience Research Institute, Peking University, Beijing 100191, China |
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| Abstract: | 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. |
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| Keywords: | 11C-carfenatnil(11C-CFN) choline module automated synthesis PET imaging |
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