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 S Vardanyan, Victor J Hruby

Research output: Contribution to journalArticlepeer-review

51 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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