Truncation of the peptide sequence in bifunctional ligands with mu and delta opioid receptor agonist and neurokinin 1 receptor antagonist activities

Padma Nair, Takashi Yamamoto, Tally M. Largent-Milnes, Scott Cowell, Vinod Kulkarni, Sharif Moye, Edita Navratilova, Peg Davis, Shou Wu Ma, Todd W. Vanderah, Josephine Lai, Frank Porreca, Victor J. Hruby

Research output: Contribution to journalArticle

8 Scopus citations

Abstract

The optimization and truncation of our lead peptide-derived ligand TY005 possessing eight amino-acid residues was performed. Among the synthesized derivatives, NP30 (Tyr1-DAla2-Gly3-Phe 4-Gly5-Trp6-O-[3′,5′-Bzl(CF 3)2]) showed balanced and potent opioid agonist as well as substance P antagonist activities in isolated tissue-based assays, together with significant antinociceptive and antiallodynic activities in vivo.

Original languageEnglish (US)
Pages (from-to)4975-4978
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume23
Issue number17
DOIs
StatePublished - Sep 1 2013

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Keywords

  • Bifunctional compounds
  • NMR structure
  • Neutokinin-1 receptor antagonists
  • Opioid receptor agonists
  • Truncation of peptide sequence

ASJC Scopus subject areas

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

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