Binding of 5-(2′-[18F]fluoroenthyl)flumazenil to central benzodiazepine receptors measured in living baboon by positron emission tomography

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Abstract

5-(2′-[18F]Fluoroethyl)flumazenil ([18F]FEF), a fluorine-18-labeled analogue of the benzodiazepine antagonist flumazenil, was evaluated for use with positron emission tomography (PET). PET imaging of a baboon after i.v. injection of [18F]FEF showed that the radiofluorinated ligand rapidly localized in vivo within benzodiazepine receptor-rich cerebral tissues, and that selective disposition was retained for over 2 h. Coinjection of unlabeled flumazenil (0.55 mg/kg i.v.) abolished the heterogeneous cerebral distribution of the tracer; receptor-specific uptake was reduced by approximately 95%. The fluorinated benzodiazepine antagonist was degraded in vivo only to polar radiometabolites that do not cross the blood-brain barrier. [18F]FEF has advantages over existing PET radiopharmaceuticals, and is a promising radioligand for non-invasive evaluation of central benzodiazepine receptor binding in vivo.

Original languageEnglish
Pages (from-to)109-115
Number of pages7
JournalEuropean Journal of Pharmacology
Volume218
Issue number1
DOIs
StatePublished - Jul 21 1992

Keywords

  • Benzodiazepine receptors
  • Flumazenil
  • Imaging
  • Neuroreceptors
  • PET (positron emission tomography)
  • [F]FEF (5-(2′-[F]Fluoroethyl)flumazenil)

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