Solid-phase synthetic strategy and bioevaluation of a labeled δ-opioid receptor ligand Dmt-Tic-Lys for In Vivo imaging

Jatinder S. Josan, David L. Morse, Liping Xu, Maria Trissal, Brenda Baggett, Peg Davis, Josef Vagner, Robert J. Gillies, Victor J. Hruby

Research output: Contribution to journalArticle

19 Scopus citations

Abstract

A general solid-phase synthetic strategy is developed to prepare fluorescent and/or lanthanide-labeled derivatives of the δ-opioid receptor (δOR) ligand H-Dmt-Tic-Lys(R)-OH. The high δ-OR affinity {K i = 3 nM) and desirable in vivo characteristics of the Cy5 derivative 1 suggest its usefulness for structure - function studies and receptor localization and as a high-contrast noninvasive molecular marker for live imaging ex vivo or in vivo.

Original languageEnglish (US)
Pages (from-to)2479-2482
Number of pages4
JournalOrganic Letters
Volume11
Issue number12
DOIs
StatePublished - Jun 18 2009

ASJC Scopus subject areas

  • Biochemistry
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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