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

A new AChE tracer N-[ super(11)C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2- (2',2'-diphenylpropionoxymethyl)pyridinium ([ super(11)C]MDDP, [ super(11)C]1) has been synthesized in 40-65% radiochemical yield. Initial PET dynamic studies of [ super(11)C]MDDP in rat heart showed rapid heart up...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-10, Vol.15 (20), p.4510-4514
Main Authors: Wang, Ji-Quan, Miller, Michael A, Mock, Bruce H, Lopshire, John C, Groh, William J, Zipes, Douglas P, Hutchins, Gary D, Zheng, Qi-Huang
Format: Article
Language:English
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Summary:A new AChE tracer N-[ super(11)C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2- (2',2'-diphenylpropionoxymethyl)pyridinium ([ super(11)C]MDDP, [ super(11)C]1) has been synthesized in 40-65% radiochemical yield. Initial PET dynamic studies of [ super(11)C]MDDP in rat heart showed rapid heart uptake and blood pool clearance to give high-quality heart images. Blocking studies of [ super(11)C]MDDP with pretreatment drug neostigmine in rats found only minor reductions in rat heart [ super(11)C]MDDP retention. The results suggest that [ super(11)C]MDDP delineates the heart very clearly, and the uptakes of [ super(11)C]MDDP in rat heart might be related to non-specific binding.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.07.034