Synthesis and preliminary evaluation of [18F]FEtP4A, a promising PET tracer for mapping acetylcholinesterase in vivo

Nucl Med Biol. 2002 May;29(4):463-8. doi: 10.1016/s0969-8051(01)00315-8.

Abstract

N-[18F]Fluoroethyl-4-piperidyl acetate ([18F]FEtP4A), an analog of [11C]MP4A for mapping brain acetylcholineseterase (AchE) activity, was prepared by reacting 4-piperidyl acetate (P4A) with [18F]fluoroethyl bromide ([18F]FEtBr) using a newly developed automated system. Preliminary evaluation showed that the initial uptake of [18F]FEtP4A in the mouse brain was > 8% injected dose/g tissue. The distribution pattern of [18F]FEtP4A in the brain was striatum>cerebral cortex>cerebellum within 10-120 min post-injection, which reflected the distribution rank pattern of AchE activity in the brain. Moreover, chemical analysis of in vivo radioactive metabolites in the mouse brain indicated that 83% of [18F]FEtP4A was hydrolyzed to N-[18F]fluoroethyl-4-piperidinol ([18F]FEtP4OH) after 1 min intravenous injection. From these results, [18F]FEtP4A may become a promising PET tracer for mapping the AchE in vivo.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetates / chemical synthesis*
  • Acetates / pharmacokinetics*
  • Acetylcholinesterase / metabolism*
  • Animals
  • Brain / diagnostic imaging
  • Brain / metabolism*
  • Cerebellum / diagnostic imaging
  • Cerebellum / metabolism
  • Cerebral Cortex / diagnostic imaging
  • Cerebral Cortex / metabolism
  • Corpus Striatum / diagnostic imaging
  • Corpus Striatum / metabolism
  • Fluorine Radioisotopes / pharmacokinetics*
  • Mice
  • Piperidines / chemical synthesis*
  • Piperidines / pharmacokinetics*
  • Radionuclide Imaging
  • Sensitivity and Specificity
  • Tissue Distribution

Substances

  • Acetates
  • Fluorine Radioisotopes
  • N-fluoroethyl-4-piperidyl acetate
  • Piperidines
  • Acetylcholinesterase