A novel photoaffinity label for the dopamine transporter based on N-substituted 3α-[bis(4'-fluorophenyl)methoxy]tropane

Gregory E. Agoston, Roxanne Vaughan, John R. Lever, Sari Izenwasser, Phyllis D. Terry, Amy Hauck Newman

Research output: Contribution to journalArticle

18 Scopus citations

Abstract

A novel photoaffinity label for the dopamine transporter (DAT) based on N-substituted 3α-[bis(4'-fluorophenyl)methoxy] tropane has been synthesized in five steps and has been characterized. Preliminary binding studies indicated this ligand bound irreversibly to the dopamine transporter. Preparation of the 125I analog and its photoactivation in the presence of membrane bound DAT demonstrated it covalently binds to the DAT.

Original languageEnglish (US)
Pages (from-to)3027-3032
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume7
Issue number23
DOIs
StatePublished - Dec 2 1997
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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