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

页码：51 / 59

页数：9

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