Automated Synthesis of 5-HT1A Receptors Antagonists 11C-WAY-100635
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-deme...
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Published in | Tong wei su Vol. 30; no. 2; pp. 119 - 124 |
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Main Author | |
Format | Journal Article |
Language | Chinese |
Published |
Editorial Board of Journal of Isotopes
01.02.2017
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Subjects | |
Online Access | Get full text |
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Summary: | 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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ISSN: | 1000-7512 1000-7512 |
DOI: | 10.7538/tws.2016.youxian.036 |