Synthesis and evaluation of 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-[11C]ethyl-1,3-dihydro-2H-benzimidazol-2-one as a brain ORL1 receptor imaging agent for positron emission tomography

被引：12
|
作者：
Ogawa, M
Hatano, K [1 ]
Kawasumi, Y
Ishiwata, K
Kawamura, K
Ozaki, S
Ito, K
机构：
[1] Natl Inst Longev Sci, Dept Biofunct Res, Obu 4748522, Japan
[2] Tokyo Metropolitan Inst Gerontol, Positron Med Ctr, Tokyo 1730022, Japan
[3] Banyu Pharmaceut Co Ltd, Banyu Tsukuba Res Inst, Merck Res Labs, Tsukuba, Ibaraki 3002611, Japan
来源：
NUCLEAR MEDICINE AND BIOLOGY | 2003年 / 30卷 / 01期
关键词：
C-11]CPEB; ORL1; receptor; nociceptin; positron emission tomography; central nervous system;
D O I：
10.1016/S0969-8051(02)00352-9
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：
1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-[C-11]ethyl-1,3-dihydro-2H-benzimidazol-2-one ([C-11]CPEB) was synthesized by [C-11]N-ethylation and evaluated as a potential brain OPL1 receptor imaging agent by positron emission tomography. The uptake of [C-11]CPEB in the mouse brain was 1.9% dose/g, 2 min post-injection, and gradually decreased with time. Receptor-specific binding was observed, however, the contribution of other receptors was observed and the non-specific binding of [C-11]CPEB was too high for imaging receptors in vivo. Therefore, [C-11]CPEB is not a suitable tracer for in vivo ORL1 receptor imaging. (C) 2002 Elsevier Science Inc. All rights reserved.
引用
收藏
页码：51 / 59
页数：9
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