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

被引：34
|
作者：
Yanamoto, Kazuhiko [1 ]
Kumata, Katsushi [1 ]
Yamasaki, Tomoteru [1 ]
Odawara, Chika [1 ]
Kawamura, Kazunori [1 ]
Yui, Joji [1 ]
Hatori, Akiko [1 ]
Suzuki, Kazutoshi [1 ]
Zhang, Ming-Rong [1 ]
机构：
[1] Natl Inst Radiol Sci, Mol Imaging Ctr, Dept Mol Probes, Inage Ku, Chiba 2638555, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 06期
关键词：
Positron emission tomography; Fluorine-18; Peripheral-type benzodiazepine receptor; 18F]FEAC; 18F]FEDAC; PRIMATE BRAIN; PET LIGAND; BINDING; RATS; NEUROINFLAMMATION; RADIOLIGAND; BROMIDE; PROTEIN; DISEASE;
D O I：
10.1016/j.bmcl.2009.01.093
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
[F-18]FEAC ([F-18]4a) and [F-18]FEDAC ([F-18]4b) were developed as two novel positron emission tomography (PET) ligands for peripheral-type benzodiazepine receptor (PBR). [F-18]4a and [F-18]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. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1707 / 1710
页数：4
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