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 Citations (Scopus)

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 - 1997

Fingerprint

Opioid Peptides
Bioactivity
Somatostatin
Biological Assay
Analgesia
Opioid Analgesics
Tail
Signal Transduction
Signal transduction
Water
Bioassay
Brain
Isomers
Rats
Assays
Therapeutics
CTAP octapeptide

Keywords

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

ASJC Scopus subject areas

  • Biochemistry
  • Endocrinology
  • Physiology
  • Cellular and Molecular Neuroscience

Cite this

Opioid peptides : Simultaneous δ agonism and μ antagonism in somatostatin analogues. / Bonner, G. Gregg; Davis, Peg; Stropova, Dagmar; Ferguson, Ron; Yamamura, Henry I.; Porreca, Frank; Hruby, Victor J.

In: Peptides, Vol. 18, No. 1, 1997, p. 93-100.

Research output: Contribution to journalArticle

Bonner, G. Gregg ; Davis, Peg ; Stropova, Dagmar ; Ferguson, Ron ; Yamamura, Henry I. ; Porreca, Frank ; Hruby, Victor J. / Opioid peptides : Simultaneous δ agonism and μ antagonism in somatostatin analogues. In: Peptides. 1997 ; Vol. 18, No. 1. pp. 93-100.
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