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[18F]FMDAA1106 and [18F]FEDAA1106:: Two positron-emitter labeled ligands for peripheral benzodiazepine receptor (PBR)

被引：87
作者：
Zhang, MR
Maeda, J
Furutsuka, K
Yoshida, Y
Ogawa, M
Suhara, T
Suzuki, K
机构：
[1] Natl Inst Radiol Sci, Dept Med Imaging, Inage Ku, Chiba 2638555, Japan
[2] SHI Accelerator Serv Co Ltd, Shinagawa Ku, Tokyo 1418686, Japan
[3] Japa Sci & Technol Corp, CREST, Kawaguchi 3320012, Japan
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 02期
关键词：
D O I：
10.1016/S0960-894X(02)00886-7
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
We synthesized and evaluated N-(5-fluoro-2-phenoxyphenyl)-N-(2-[F-18]fluoromethyl-5-methoxybenzyl)acetamide ([F-18]FMDAA1106) and N-(5-fluoro-2-phenoxyphenyl)-N-(2-[F-18]fluoroethyl-5-methoxybenzyl)acetamide ([F-18]FEDAA1106) as two potent radioligands for peripheral benzodiazepine receptors (PBR). [F-18]FMDAA1106 and [F-18]FEDAA1106 were respectively synthesized by fluoroalkylation of the desmethyl precursor DAA1123 with [F-18]FCH2I and [F-18]FCH2CH2Br. Ex vivo autoradiograms of [F-18]FMDAA1106 and [F-18]FEDAA1106 binding sites in the rat brains revealed that a high radioactivity was present in the olfactory bulb, the highest PBR density region in the brain. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：201 / 204
页数：4
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