摘要
目的：研发全自动化一步法（11C）标记水通道蛋白抑制剂显像剂。材料与方法：在TRACERlab FXC合成仪平台上，碱性条件下（11C）CH3I与乙酰唑胺在100℃条件下反应。然后以磷酸二氢钠为淋洗液，通过高性能液体色谱（High performance liquid chromatography，HPLC）分离获得（11C）N-甲基乙酰唑胺。结果：合成效率在50％以上，放射化学纯度>98％，整个合成过程大约30 min。（11C）N-甲基乙酰唑胺PET/CT大鼠扫描获得（11C）N-甲基乙酰唑胺在大鼠体内分布，通过乙酰唑胺抑制剂抑制后，（11C）N-甲基乙酰唑胺在大鼠肝脏摄取明显降低。结论：（11C）N-甲基乙酰唑胺能够作为水通道蛋白显像剂。
Abstract
Objective: To research and synthesize the fully automated one-step (11C) labeled water channel protein(AQP) inhibitor, the imaging agent. Materials and Methods: Using the TRACERlab FXC synthesis platform, under 100℃ reaction conditions in alkaline conditions (11C) CH3I reacted with acetazolamide. Then using sodium biphosphate as eluent, through high performance liquid chromatography(HPLC), (11C)N-methylacetazolamide was isolated from reaction solution. Results: The synthesis efficiency of the agent was above 50%, the radiochemical purity was over 98%, the time for the whole producing process was only about 30 min. After intravenous injection of (11C)N-methylacetazolamide into the tail vein of rat, and performing PET/CT scanning, the distribution of the above agent can be seen in rats, after injection of (11C)N-methylacetazolamide and N-methylacetazolamide, the inhibitor, the (11C)N-methylacetazolamide decreased significantly in the rat is liver. Conclusion: This is the first study and report on development of the fully automated one-step (11C) labeled water channel protein(AQP) inhibitor. The (11C)N-methylacetazolamide can be used as AQP PET tracer agent.
关键词
放射性药物 /
乙酰唑胺 /
正电子发射断层显像术
Key words
Radiopharmaceuticals /
Acetazolamide /
Positron-emission tomography
曹 礼;杜 名;张 新;李宏利;韩婷婷;赵周社;辛 军;郭启勇.
（11C）标记水通道蛋白抑制显像剂全自动合成方法[J]. 中国临床医学影像杂志. 2014, 25(5): 344-346
CAO Li;DU Ming;ZHANG Xin;LI Hong-li;HAN Ting-ting;ZHAO Zhou-she;XIN Jun;GUO Qi-yong.
Research on producing fully automated one-step (11C) labeled water channel protein inhibitor, the imaging agent[J]. Journal of China Clinic Medical Imaging. 2014, 25(5): 344-346
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