Fluoro-norchloroepibatidine: Preclinical assessment of acute toxicity

Patricia E. Molina, Yu Shin Ding, F. Ivy Carroll, F. Liang, Nora D. Volkow, Naomi Pappas, Michael Kuhar, Naji Abumrad, S. John Gatley, Joanna S. Fowler

Research output: Contribution to journalArticlepeer-review

70 Scopus citations

Abstract

18Fluoro-norchloroepibatidine (exo-2-(6-fluoro-3-pyridyl)-7- azabicyclo-[2.2.1]heptane [NFEP]), a labeled derivative of epibatidine, has shown promise for imaging brain nicotinic acetylcholine receptors with PET. We determined the dose-dependent effects of NFEP in conscious rats. NFEP (1.5 μg/kg; administered intravenously) resulted in 30% mortality. Neither 0.5 μg/kg or 0.25 μg/kg NFEP resulted in any significant changes in cardiorespiratory parameters, but plasma catecholamines increased (2- to 3- fold). Further studies are needed to determine the safety of NFEP that are specifically designed to assess the catecholamine response. Our results suggest that it is not advisable to initiate human PET studies with [18F]- NFEP without further evidence supporting its safety.

Original languageEnglish
Pages (from-to)743-747
Number of pages5
JournalNuclear Medicine and Biology
Volume24
Issue number8
DOIs
StatePublished - Nov 1997
Externally publishedYes

Keywords

  • Fluoro-norchloroepibatidine
  • Hemodynamics
  • Nicotinic acetylcholine receptors
  • Positron emission tomography
  • Toxicity

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