Development of novel enkephalin analogues that have enhanced opioid activities at both μ and δ opioid receptors

Sun Lee Yeon, Ravil Petrov, Chad K. Park, Shou Wu Ma, Peg Davis, Josephine Lai, Frank Porreca, Ruben Vardanyan, Victor J. Hruby

Research output: Contribution to journalArticle

31 Scopus citations

Abstract

Enkephalin analogues with a 4-anilidopiperidine scaffold have been designed and synthesized to achieve therapeutic benefit for the treatment of pain due to mixed μ and δ opioid agonist activities. Ligand 16, in which a Dmt-substituted enkephalin-like structure was linked to the N-phenyl-N- piperidin-4-yl propionamide moiety, showed very high binding affinities (0.4 nM) at μ and δ receptors with an increased hydrophobicity (aLogP = 2.96). This novel lead compound was found to have very potent agonist activities in MVD (1.8 nM) and GPI (8.5 nM) assays.

Original languageEnglish (US)
Pages (from-to)5528-5532
Number of pages5
JournalJournal of Medicinal Chemistry
Volume50
Issue number22
DOIs
StatePublished - Nov 1 2007

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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