首都医科大学学报 ›› 2008, Vol. 29 ›› Issue (1): 8-11.

• 专题报道 • 上一篇    下一篇

全自动合成3-18F-2-羟基丙烷-2-硝基咪唑及临床前研究

张锦明1, 郑昕2, 柳羲2, 郭喆1, 刘晓飞1, 田嘉禾1   

  1. 1. 中国人民解放军总医院核医学科;2. 中国人民解放军总医院胸外科
  • 收稿日期:2007-11-18 修回日期:1900-01-01 出版日期:2008-02-24 发布日期:2013-07-15

Fully Automated Synthesis of [18F]Fluoromisonidazole and Preclinical Study

Zhang Jinming1, Zheng Xin2, Liu Xi2, Guo Zhe1, Liu Xiaofei1, Tian Jiahe1   

  1. 1. Department of Nuclear Medicine, General Hospital of PLA;2. Department of Thoracic Surgery, General Hospital of PLA
  • Received:2007-11-18 Revised:1900-01-01 Online:2008-02-24 Published:2013-07-15

摘要: 目的 研究一种全自动合成肿瘤乏氧显像剂3-18F-2-羟基丙烷-2-硝基咪唑(18F-FMISO)的方法.方法 采用改良的FDG(氟代脱氧葡萄糖)模块,在密闭体系下4~6 mg前体与F-18离子在110 ℃反应300 s,1 mol/L HCl 120 ℃下水解180 s,经柱色层纯化得18F-FMISO.检测正常小鼠、荷瘤鼠的生物学分布及PET显像.结果 采用FDG模块自动化合成18F-FMISO,合成效率为67%,时间为25 min,放化纯度>99%,体外稳定性良好.生物学分布及PET显像表明,肿瘤明显摄取18F-FMISO,120 min时瘤/肌比为2.99, 但肝、肾、肠的放射性较高.结论 改良的FDG模块可高效、快速合成18F-FMISO,其产品质量符合临床要求.18F-FMISO适于胸、颈部肿瘤的乏氧评价.

关键词: 18F-FMISO, 自动化合成, 肿瘤乏氧, PET显像

Abstract: Objective To study a new fully automated method for the synthesis of [18F]fluoromisonidazole(18F-FMISO) by a home made FDG synthesizer.Methods The optimal labeling conditions for the automated synthesis of 18F-FMISO was 4~6 mg precursor in 1 mL acetonitrile heated at 110 ℃ for 300 s at pressurized vessel,and hydrolyzed with 1 mol/L HCl at 120 ℃ for 180 s with modified FDG synthesizer.The biodistribution and PET scan were performed in normal and lung tumor bearing mice.Results The yield of 18F-FMISO was 67% with modified FDG module.It took 25 min.The radiochemical purity was over 99%.The stabilization of 18F-FMISO was good in vitro.The PET scan showed that the tumor took up 18F-FMISO.The ratio of tumor to muscle was 2.99 at 120 min.The liver,kidney and intestines took up 18F-MISO abundantly.Conclusion The modified FDG module can be used for synthesis of high yield 18F-FMISO.It could be used in clinical practice as a potential radiopharmaceutical for the non-invasive detection of hypoxia in thorax and neck tumors.

Key words: 18F-FMISO, automated synthesis, tumor hypoxia, PET imaging

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