[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

页码：1707 / 1710

页数：4

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