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

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4510-4. doi: 10.1016/j.bmcl.2005.07.034.

Abstract

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

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetylcholinesterase / blood
  • Acetylcholinesterase / metabolism*
  • Animals
  • Brain / enzymology
  • Butyrylcholinesterase / blood
  • Butyrylcholinesterase / metabolism
  • Myocardium / enzymology*
  • Positron-Emission Tomography
  • Pyridinium Compounds / chemical synthesis*
  • Pyridinium Compounds / chemistry*
  • Rats

Substances

  • N-(11C)methyl-3-(((dimethylamino)carbonyl)oxy)-2-(2',2'-diphenylpropionoxymethyl)pyridinium
  • Pyridinium Compounds
  • Acetylcholinesterase
  • Butyrylcholinesterase