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

Ji Quan Wang, Michael A. Miller, Bruce H. Mock, John C. Lopshire, William Groh, Douglas P. Zipes, Gary Hutchins, Qi-Huang Zheng

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)4510-4514
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume15
Issue number20
DOIs
StatePublished - Oct 15 2005

Fingerprint

Acetylcholinesterase
Imaging techniques
Rats
Neostigmine
N-(11C)methyl-3-(((dimethylamino)carbonyl)oxy)-2-(2',2'-diphenylpropionoxymethyl)pyridinium
Blood
Pharmaceutical Preparations

Keywords

  • Acetylcholinesterase
  • Heart
  • N-[C]methyl-3-[[(dimethylamino)carbonyl]oxy]-2-(2′, 2′-diphenylpropionoxymethyl)pyridinium
  • Positron emission tomography
  • Synthesis
  • Tracer

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Organic Chemistry
  • Drug Discovery
  • Pharmaceutical Science

Cite this

Facile synthesis and PET imaging of a novel potential heart acetylcholinesterase tracer N-[11C]methyl-3-[[(dimethylamino) carbonyl]oxy]-2-(2′,2′-diphenylpropionoxymethyl)pyridinium. / Wang, Ji Quan; Miller, Michael A.; Mock, Bruce H.; Lopshire, John C.; Groh, William; Zipes, Douglas P.; Hutchins, Gary; Zheng, Qi-Huang.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 15, No. 20, 15.10.2005, p. 4510-4514.

Research output: Contribution to journalArticle

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abstract = "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.",
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AU - Mock, Bruce H.

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AU - Zipes, Douglas P.

AU - Hutchins, Gary

AU - Zheng, Qi-Huang

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