Facile synthesis and PET imaging of a novel potential heart acetylcholinesterase tracer N-[¹¹C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2′,2′-diphenylpropionoxymethyl)pyridinium

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• 作者：Ji-Quan Wang ; Michael A. Miller ; Bruce H. Mock ; John C. Lopshire ; William J. Groh ; Douglas P. Zipes ; Gary D. Hutchins and Qi-Huang Zheng
• 关键词：N-[¹¹C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2′ ; 2′ ; -diphenylpropionoxymethyl)pyridinium ; Tracer ; Synthesis ; Positron emission tomography ; Acetylcholinesterase ; Heart
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：2005
• 卷：15
• 期：20
• 页码：4510-4514
• 文件大小：165 K

摘要

A new AChE tracer N-[¹¹C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2′,2′-diphenylpropionoxymethyl)pyridinium ([¹¹C]MDDP, [¹¹C]1) has been synthesized in 40–65%radiochemical yield. Initial PET dynamic studies of [¹¹C]MDDP in rat heart showed rapid heart uptake and blood pool clearance to give high-quality heart images. Blocking studies of [¹¹C]MDDP with pretreatment drug neostigmine in rats found only minor reductions in rat heart [¹¹C]MDDP retention. The results suggest that [¹¹C]MDDP delineates the heart very clearly, and the uptakes of [¹¹C]MDDP in rat heart might be related to non-specific binding.