5-HT_(1A)受体拮抗剂~(11)C-WAY-100635的自动化合成

为自动化合成用于5-羟色胺(5-HT_(1A))受体显像~(11)C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(~(11)C-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~(11)C-WAY-100635注射液。结果显示,合成方法共耗时约40 min,~(11)C-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~(11)C-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-HT_(1A)受体显像剂~(11)C-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。

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

A fully automated synthesis of 11C-labeled N-[2-[4-(2-methoxyphenyl)-l-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 of11C-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.