Synthesis and evaluation of 11C- and 18F-labeled 1-[2-(4-alkoxy-3-methoxyphenyl)ethyl]-4-(3-phenylpropyl)piperazines as sigma receptor ligands for positron emission tomography studies

被引:52
作者
Kawamura, K [1 ]
Elsinga, PH
Kobayashi, T
Ishii, S
Wang, WF
Matsuno, K
Vaalburg, W
Ishiwata, K
机构
[1] Tokyo Metropolitan Inst Gerontol, Positron Med Ctr, Tokyo, Japan
[2] SHI Accelerator Serv Ltd, Tokyo, Japan
[3] Univ Groningen Hosp, PET Ctr, Groningen, Netherlands
[4] Ms Sci Co, Kobe, Hyogo, Japan
[5] Santen Pharmaceut Co Ltd, Nara Res & Dev Ctr, Ikoma, Japan
关键词
sigma receptor; positron emission tomography; SA4503; SA5845;
D O I
10.1016/S0969-8051(02)00439-0
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 prepared sigma(1)-receptor selective 1-([4-methoxy-C-11]-3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine ([C-11]SA4503) and its fluorinated analog 1-([4-methoxy-C-11]3,4-dimethoxyphenethyl)-4-[3-(4-fluorophenyl)propyl]piperazine ([C-11]SA5845), and their [C-11]ethoxy and [F-18]fluoroethoxy analogs, and evaluated their potential for positron emission tomography studies. [C-11]SA4503 is most selective for sigma(1) receptors. and the other five showed affinities for sigma(1) and sigma(2) receptors with a different extent. All radioligands showed the receptor-specific binding in the brain, and Visualized similar regional brain distributions by ex vivo autoradiography. The [C-11]ethoxy analogs were relatively labile for metabolism. (C) 2003 Elsevier Science Inc. All rights reserved.
引用
收藏
页码:273 / 284
页数:12
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