6-[18F]fluoro-A-85380: An in vivo tracer for the nicotinic acetylcholine receptor

Ursula Scheffel, Andrew G. Horti, Andrei O. Koren, Hayden T. Ravert, Jeffrey P. Banta, Paige A. Finley, Edythe D. London, Robert F. Dannals

Research output: Contribution to journalArticle

Abstract

6-[18F]Fluoro-3-(2(S)-azetidinylmethoxy)pyridine (6-[18F]fluoro-A-85380 or 6-[18F]FA), a new tracer for positron emission tomography, was synthesized by no-carrier-added [18F] fluorination of 6-iodo-3-((1-tert-butoxycarbonyl-2(S)-azetidinyl)methoxy)pyridine followed by acidic deprotection. 6-[18F]FA followed the regional densities of brain nicotinic acetylcholine receptors (nAChRs) reported in the literature. Evidence of binding to nAChRs and high specificity of the binding in vivo was demonstrated by inhibition with nAChR selective ligands as well as with unlabeled 6-FA. A preliminary toxicology study of the 6-FA showed a relatively low biological effect. Copyright (C) 2000 Elsevier Science Inc.

Original languageEnglish (US)
Pages (from-to)51-56
Number of pages6
JournalNuclear Medicine and Biology
Volume27
Issue number1
DOIs
StatePublished - Jan 1 2000

Keywords

  • 6-[F]FA
  • A-85380 derivative
  • Mouse brain distribution
  • Nicotinic acetylcholine receptor (nAChR)
  • PET
  • Radiotracer

ASJC Scopus subject areas

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

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