Development of potent μ and δ opioid agonists with high lipophilicity

Yeon Sun Lee, Vinod Kulkarani, Scott M. Cowell, Shou Wu Ma, Peg Davis, Katherine E. Hanlon, Todd W. Vanderah, Josephine Lai, Frank Porreca, Ruben Vardanyan, Victor J. Hruby

Research output: Contribution to journalArticle

35 Scopus citations

Abstract

An SAR study on the Dmt-substituted enkephalin-like tetrapeptide with a N-phenyl-N-piperidin-4-ylpropionamide moiety at the C-terminal was performed and has resulted in highly potent ligands at μ and δ opioid receptors. In general, ligands with the substitution of d-Nle2 and halogenation of the aromatic ring of Phe4 showed highly increased opioid activities. Ligand 6 with good biological activities in vitro demonstrated potent in vivo antihyperalgesic and antiallodynic effects in the tail-flick assay.

Original languageEnglish (US)
Pages (from-to)382-386
Number of pages5
JournalJournal of Medicinal Chemistry
Volume54
Issue number1
DOIs
StatePublished - Jan 13 2011

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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