Syntheses and biological evaluation of 18F-labeled 3-(1-benzyl-piperidin-4-yl)-1-(1-methyl-1H-indol-3-yl) propan-1-ones for in vivo mapping of acetylcholinesterase

被引：22

作者：

Choe, YS

Oh, SJ

Shim, I

Naruto, S

Chi, DY

Kim, SE

Lee, KH

Choi, Y

Kim, BT

机构：

[1] Sungkyunkwan Univ, Sch Med, Samsung Med Ctr, Dept Nucl Med, Seoul 135710, South Korea

[2] Samsung Biomed Res Inst, Clin Res Ctr, Seoul, South Korea

[3] Sankyo Co Ltd, Exploratory Chem Res Labs, Tokyo 140, Japan

[4] Inha Univ, Dept Chem, Inchon 402751, South Korea

来源：

NUCLEAR MEDICINE AND BIOLOGY | 2000年 / 27卷 / 03期

关键词：

Alzheimer's disease; F-18; acetylcholinesterase; acetylcholinesterase inhibitor;

D O I：

10.1016/S0969-8051(00)00086-X

中图分类号：

R8 [特种医学]; R445 [影像诊断学];

学科分类号：

1002 ; 100207 ; 1009 ;

摘要：

We synthesized novel F-18-labeled acetylcholinesterase (AChE) inhibitors, 3-[1-(3- and 4-[F-18]fluoromethylbenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-ones ([F-18]1 and [F-18]2) and 3-[1-(4-[F-18]fluorobenzyl)piperidin-4-yl]-1-(1-methyl-1H-indol-3-yl)propan-1-one ([F-18]3) in high yields (decay-corrected, 25%-40%) and with high effective specific activities (>37 GBq/mu mol). Tissue distribution studies of the [F-18]1 and the [F-18]3 in mice showed the nonspecific bindings in brain regions, with metabolic defluorination of the [F-18]1. The result suggests that these radioligands may not be suitable agents for in vivo mapping of AChE, despite their potent in vitro anti-AChE activities. NUCL MED BIOL 27;3: 263-267, 2000. (C) 2000 Elsevier Science Inc. All rights reserved.

引用

页码：263 / 267

页数：5

共 18 条

[1] C-11 LABELING OF AN INHIBITOR OF ACETYLCHOLINESTERASE - [C-11] PHYSOSTIGMINE [J].