Design and evaluation of radioactive acetylcholine analogs for mapping brain acetylcholinesterase (AchE) in vivo

Nucl Med Biol. 1994 Aug;21(6):801-8. doi: 10.1016/0969-8051(94)90159-7.


For mapping brain acetylcholinesterase (AchE) in vivo, seven radioactive acetylcholine analogs, N-[14C]methylpiperidyl-3- and 4-acetates, propionates, isobutyrates, and 3-butyrate were newly synthesized and evaluated in mice. The esters readily entered the brain and were hydrolyzed into the hydrophilic metabolite, which was trapped. In brain homogenates, the esters showed a wide range of enzymatic reactivity (about 40-fold), and high specificity for AchE (more than 82%) except the butyrate. Intra-brain distribution of the esters reflected a pattern of AchE activity.

MeSH terms

  • Acetylcholine / analogs & derivatives
  • Acetylcholine / chemical synthesis
  • Acetylcholine / metabolism*
  • Acetylcholinesterase / metabolism*
  • Animals
  • Brain / blood supply
  • Brain / enzymology*
  • Carbon Radioisotopes / chemistry
  • Carbon Radioisotopes / metabolism*
  • Magnetic Resonance Spectroscopy
  • Male
  • Mice
  • Mice, Inbred C3H
  • Regional Blood Flow
  • Substrate Specificity


  • Carbon Radioisotopes
  • Acetylcholinesterase
  • Acetylcholine