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Automated Synthesis of 5-HT1A Receptors Antagonists 11C-WAY-100635

LI Hui-qiang1,2;ZHEN Zhi-fei1;ZHANG Wei-feng1;LIAO Shu-guang1;LI Hong-li3;XU Jun-ling1,2   

  1. 1.Henan Provincial People’s Hospital Department of Nuclear Medicine, Zhengzhou 450003, China;2.Department of Nuclear Medicine, the People’s Hospital of Zhengzhou University, Zhengzhou 450003, China; 3.GE Healthcare China, Beijing 100176, China
  • Online:2017-05-20 Published:2017-05-22

5-HT1A 受体拮抗剂11C-WAY-100635的自动化合成

李会强1,2;甄志飞1;张伟峰1;廖曙光1;李宏利3;徐俊玲1,2   

  1. 1.河南省人民医院 核医学科,郑州450003;2.郑州大学人民医院 核医学科,郑州450003;3.通用电气医疗集团(中国),北京100176

Abstract:

A fully automated synthesis of 11C-labeled-N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-2-pyridinylcyclohexanecarboxamide maleate  (11C-WAY-100635) for imaging 5-HT1A receptors was performed on a module system. 11C-WAY-100635 was obtained based on the methylation reaction of the precursor (O-demethyl)-WAY-100635, purification with HPLC and subsequent removal of organic solvents using a Sep-Pak Plus C18. The results revealed that fully automated synthesis of 11C-WAY-100635 was completed within the total synthesis time of about 40 min. The uncorrected radiochemical yield was between 10% and 20%, and the radiochemical purity was over 97%. After the intravenous injection of 11C-WAY-100635 (about 111 MBq), the uptake in the brain tissues of the white rabbit was significantly higher than the other tissues of head. This method provides simple synthesis of 11C-WAY-100635 with relatively short radiosynthesis time and a high radiochemical yield for clinical need.

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摘要:

为自动化合成用于5-羟色胺(5-HT1A)受体显像11C标记的N-[2-[4-(2-甲氧基苯基)-1-哌嗪基]乙基]-N-2-吡啶基环己烷甲酰胺(11C-WAY-100635),采用自动化合成模块,以去甲基WAY-100635为前体,经甲基化,HPLC纯化和Sep-Pak Plus C18柱去除有机溶剂制得11C-WAY-100635注射液。结果显示,合成方法共耗时约40 min,11C-WAY-100635注射液的未校正放化产率10%~20%,放化纯度>97%;静脉注射日本大耳白兔11C-WAY-100635(约111 MBq)后,脑组织放射性摄取显著,且明显高于头颅等其他组织。自动化合成5-HT1A受体显像剂11C-WAY-100635方法简单,反应时间较短,放化纯度高,产率稳定可靠,可在临床中推广应用。

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