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

被引：11
|
作者：
Wang, JQ
Miller, MA
Mock, BH
Lopshire, JC
Groh, WJ
Zipes, DP
Hutchins, GD
Zheng, QH [1 ]
机构：
[1] Indiana Univ, Sch Med, Dept Radiol, Indianapolis, IN 46202 USA
[2] Indiana Univ, Sch Med, Krannert Inst Cardiol, Dept Med, Indianapolis, IN 46202 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 20期
关键词：
N-[C-11]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2'; 2'diphenylpropionoxymethyl)pyridinium; tracer; synthesis; positron emission tomography; acetylcholmesterase; heart;
D O I：
10.1016/j.bmcl.2005.07.034
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A new AChE tracer N-[C-11]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2 ',2 '-diphenylpropionoxymethyl)pyridinium ([C-11]MDDP, [C-11]1) has been synthesized in 40-65% radiochemical yield. Initial PET dynamic studies of [C-11] MDDP in rat heart showed rapid heart uptake and blood pool clearance to give high-quality heart images. Blocking studies of [I C]MDDP with pretreatment drug neostigmine in rats found only minor reductions in rat heart [C-11]MDDP retention. The results suggest that [C-11]MDDP delineates the heart very clearly, and the uptakes of [C-11]MDDP in rat heart might be related to non-specific binding. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码：4510 / 4514
页数：5
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