Pharmacological evaluation of [11C]donepezil as a tracer for visualization of acetylcholinesterase by PET

Nucl Med Biol. 2000 Nov;27(8):745-7. doi: 10.1016/s0969-8051(00)00166-9.

Abstract

Donepezil is a highly potent and selective reversible achetylcholinesterase inhibitor. [(11)C]Donepezil is prepared by methylation with [(11)C]CH(3)I of the corresponding 6'-O-desmethylprecursor. Tissue distribution in mice revealed a high uptake in brain and rapid clearance from the blood. Metabolization studies in mice indicated the formation of one (11)C-labeled polar metabolite that didn't penetrate the blood-brain barrier. Regional brain distribution in rabbits didn't reflect the measured achetylcholinesterase distribution in rabbit brain.

Publication types

  • Evaluation Study

MeSH terms

  • Acetylcholinesterase / metabolism*
  • Animals
  • Binding, Competitive
  • Brain / diagnostic imaging
  • Brain / enzymology
  • Brain / metabolism
  • Carbon Radioisotopes
  • Cholinesterase Inhibitors* / pharmacokinetics
  • Donepezil
  • Female
  • Indans* / pharmacokinetics
  • Isotope Labeling
  • Male
  • Mice
  • Piperidines* / pharmacokinetics
  • Rabbits
  • Radiopharmaceuticals* / pharmacokinetics
  • Tissue Distribution
  • Tomography, Emission-Computed

Substances

  • Carbon Radioisotopes
  • Cholinesterase Inhibitors
  • Indans
  • Piperidines
  • Radiopharmaceuticals
  • Donepezil
  • Acetylcholinesterase