胆碱模块自动化合成<sup>11</sup>C-carfentanil及Micro PET显像

胆碱模块自动化合成¹¹C-carfentanil及Micro PET显像

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。

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.