5-HT1A 受体拮抗剂11C-WAY-100635的自动化合成

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

  • 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。

     

    Abstract: A fully automated synthesis of 11C-labeled-N-2-4-(2-methoxyphenyl)-1-piperazinylethyl-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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