[¹⁸F]FEAC and [¹⁸F]FEDAC: Two novel positron emission tomography ligands for peripheral-type benzodiazepine receptor in the brain

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• 作者：Kazuhiko Yanamoto ; Katsushi Kumata ; Tomoteru Yamasaki ; Chika Odawara ; Kazunori Kawamura ; Joji Yui ; Akiko Hatori ; Kazutoshi Suzuki ; Ming-Rong Zhang
• 关键词：Positron emission tomography ; Fluorine-18 ; Peripheral-type benzodiazepine receptor ; [18F]FEAC ; [18F]FEDAC
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2009
• 出版时间：15 March 2009
• 年：2009
• 卷：19
• 期：6
• 页码：1707-1710
• 全文大小：351 K

文摘

[¹⁸F]FEAC ([¹⁸F]4a) and [¹⁸F]FEDAC ([¹⁸F]4b) were developed as two novel positron emission tomography (PET) ligands for peripheral-type benzodiazepine receptor (PBR). [¹⁸F]4a and [¹⁸F]4b were synthesized by fluoroethylation of precursors 8a and 8b with [¹⁸F]FCH₂CH₂Br ([¹⁸F]9), respectively. Small-animal PET scan for a neuroinflammatory rat model showed that the two radioligands had high uptakes of radioactivity in the kainic acid-infused striatum, a brain region where PBR density was increased.