Radiosynthesis and mouse brain distribution studies of [11C] CP-126,998: A PET ligand for In vivo study of acetylcholinesterase

John L. Musachio, John E. Flesher, Ursula A. Scheffel, Paige Rauseo, John Hilton, William B. Mathews, Hayden T. Ravert, Robert F. Dannals, J. James Frost

Research output: Contribution to journalArticle

Abstract

The selective, reversible acetylcholinesterase inhibitor 5,7-Dihydro-7-methyl-3- [2-[1-(phenylmethyl]-4-piperidinyl]ethyl]-6H-pyrrolo[3,2-f]-1, 2-benzisoxazol3-6-one (CP-126,998) was labeled with C-11 iodomethane via base-promoted alkylation of the lactam nitrogen. [11C] CP-126,998 was synthesized in good radiochemical yield (13-29% non-decay corrected) and high specific radioactivity (177-418 GBq/μmol). In vivo mouse biodistribution studies reveal [11C] CP-126,998 to localize preferentially in striatal tissue, a region known to be rich in acetylcholinesterase. Competitive blocking studies using a variety of acetylcholinesterase inhibitors (diisopropylfluorophosphate, tacrine, CP-118,954) verified the specificity of the PET radiotracer for brain acetylcholinesterase.

Original languageEnglish (US)
Pages (from-to)547-552
Number of pages6
JournalNuclear Medicine and Biology
Volume29
Issue number5
DOIs
StatePublished - Jul 2 2002

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Keywords

  • Acetylcholinesterase
  • Alzheimer's disease
  • C-11
  • Diisopropylfluorophosphate
  • PET

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

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