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

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• 作者：Ogawa ; Mikako ; Hatano ; Kentaro ; Kawasumi ; Yasuhiro ; Ishiwata ; Kiichi ; Kawamura ; Kazunori ; Ozaki ; Satoshi ; et. al.
• 关键词：[¹¹C]CPEB ; ORL1 receptor ; Nociceptin ; Positron emission tomography ; Central nervous system
• 刊名：Nuclear Medicine and Biology
• 出版年：2003
• 出版时间：January, 2003
• 年：2003
• 卷：30
• 期：1
• 页码：51-59
• 全文大小：303 K

文摘

1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-[¹¹C]ethyl-1,3-dihydro-2H-benzimidazol-2-one ([¹¹C]CPEB) was synthesized by [¹¹C]N-ethylation and evaluated as a potential brain ORL1 receptor imaging agent by positron emission tomography. The uptake of [¹¹C]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 [¹¹C]CPEB was too high for imaging receptors in vivo. Therefore, [¹¹C]CPEB is not a suitable tracer for in vivo ORL1 receptor imaging.