Opioid peptides: Simultaneous δ agonism and μ antagonism in somatostatin analogues

G. Gregg Bonner, Peg Davis, Dagmar Stropova, Ron Ferguson, Henry I. Yamamura, Frank Porreca, Victor J. Hruby

Research output: Contribution to journalArticle

16 Scopus citations

Abstract

Four isomers of the Somatostatin analogue H-D-Phe-Cys-Tyr-D-Trp-Arg-Thr-Pen-Thr-NH2 (CTAP) were made with β-MePhe in position 1 and assayed for opioid binding in rat brain, biological activity in MVD and GPI bioassays, and antinociception in mouse warm-water tail flick assays. These analogues displayed varying potencies and biological activities including: simultaneous δ receptor agonism/μ receptor antagonism, μ receptor antagonism, and δ receptor agonism. These analogues demonstrated that the N-terminal residue is important for receptor potency/selectivity and signal transduction. These analogues may represent leads to therapeutic agents that yield analgesia via δ agonist effects, yet lack side effects associated with μ activity.

Original languageEnglish (US)
Pages (from-to)93-100
Number of pages8
JournalPeptides
Volume18
Issue number1
DOIs
StatePublished - May 16 1997

Keywords

  • CTAP
  • GPI
  • MVD
  • agonist
  • analgesia
  • antagonist
  • antinocic eption
  • convulsions
  • opioid
  • somatostatin
  • β-MePhe

ASJC Scopus subject areas

  • Biochemistry
  • Physiology
  • Endocrinology
  • Cellular and Molecular Neuroscience

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