胆碱模块自动化合成11C-carfentanil及Micro PET显像

doi:10.7538/tws.2011.24.03.0182

同位素 ›› 2011, Vol. 24 ›› Issue (3): 182-187.DOI: 10.7538/tws.2011.24.03.0182

• 放射性药物和标记化合物 • 上一篇下一篇

胆碱模块自动化合成¹¹C-carfentanil及Micro PET显像

张锦明¹;徐志红²;张晓军¹;向晓辉³;田嘉禾¹

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

收稿日期:1900-01-01 修回日期:1900-01-01 出版日期:2011-08-20 发布日期:2011-08-20

Automated Synthesis of ¹¹C-carfentanil With¹¹C-choline Module and Micro PET Imaging

ZHANG Jin-ming¹;XU Zhi-hong²;ZHANG Xiao-jun¹;XIANG Xiao-hui³;TIAN Jia-he¹

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

Received:1900-01-01 Revised:1900-01-01 Online:2011-08-20 Published:2011-08-20

摘要/Abstract

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，¹¹CH_3-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。

关键词: ¹¹C-carfentanil(¹¹C-CFN), 胆碱模块, 自动化合成, PET显像

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.

Key words: ¹¹C-carfenatnil(¹¹C-CFN), choline module, automated synthesis, PET imaging

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, 24(3): 182-187.

ZHANG Jin-ming;XU Zhi-hong;ZHANG Xiao-jun;XIANG Xiao-hui;TIAN Jia-he. Automated Synthesis of ¹¹C-carfentanil With¹¹C-choline Module and Micro PET Imaging[J]. Journal of Isotopes, 2011, 24(3): 182-187.

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胆碱模块自动化合成¹¹C-carfentanil及Micro PET显像

Automated Synthesis of ¹¹C-carfentanil With¹¹C-choline Module and Micro PET Imaging

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