Spinal antinociception by Tyr-D-Ser(otbu)-Gly-Phe-Leu-Thr, a selective delta-opioid receptor agonist

Eur J Pharmacol. 1992 May 27;216(1):97-101. doi: 10.1016/0014-2999(92)90214-o.

Abstract

The spinal antinociceptive potency of the delta-opioid receptor agonist, Tyr-D-Ser(otbu)-Gly-Phe-Leu-Thr (DSTBULET), was studied in rats. The tail flick test was used as nociceptive stimulus and the rotarod test was used to detect any motor or sedative effects. A dose-response curve was also made for the mu-opioid receptor agonist, morphine. The ED50 for DSTBULET was 0.3 micrograms (0.4 nmol) and a near 100% maximum effect was achieved with 5 micrograms (7.5 nmol). No motor or sedative effects were detected. Antinociception by DSTBULET was antagonized by s.c. naltrindole (1 mg/kg), a selective delta-opioid receptor antagonist, and naloxone (1 mg/kg), a non-selective opioid receptor antagonist. The ED50 for morphine was 0.5 micrograms (1.0 nmol) and the antinociceptive effects were not antagonized by naltrindole (1 mg/kg). The results evidence further the important role of the delta-opioid receptor in spinal nociceptive processing.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Analgesics / administration & dosage
  • Analgesics / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Indoles / pharmacology
  • Injections, Spinal
  • Male
  • Molecular Sequence Data
  • Morphinans / pharmacology
  • Morphine / pharmacology
  • Naloxone / pharmacology
  • Naltrexone* / analogs & derivatives*
  • Narcotic Antagonists / pharmacology
  • Oligopeptides / administration & dosage
  • Oligopeptides / pharmacology*
  • Rats
  • Rats, Inbred Strains
  • Receptors, Opioid / metabolism*
  • Receptors, Opioid, delta

Substances

  • Analgesics
  • Indoles
  • Morphinans
  • Narcotic Antagonists
  • Oligopeptides
  • Receptors, Opioid
  • Receptors, Opioid, delta
  • tyrosyl-seryl(O-tert-butyl)-glycyl-phenylalanyl-leucyl-threonine
  • Naloxone
  • Naltrexone
  • Morphine
  • naltrindole