Agonist and antagonist effects of dynorphin A-(1-13) in a thermal antinociception assay in rhesus monkeys

J Pharmacol Exp Ther. 1995 Oct;275(1):374-80.

Abstract

The agonist and antagonist effects of intravenously administered dynorphin A-(1-13) were characterized in the warm water (50 and 55 degrees C) tail withdrawal assay of antinociception in rhesus monkeys. The peptide dose-dependently elevated tail withdrawal latencies in 50 degrees C water, but was ineffective in 55 degrees C water. The antinociceptive effect of dynorphin was surmountably antagonized by quadazocine (0.1 mg/kg) and nor-binaltorphimine (3.2 mg/kg), but was not antagonized by clocinnamox (0.1 mg/kg); this pattern of antagonism is consistent with a kappa-opioid receptor mediated effect. Pretreatment with dynorphin A-(1-13) (0.032-3.2 mg/kg) antagonized the antinociceptive effects of U50,488 and U69,593 in 55 degrees C water, suggesting a low efficacy action of the peptide at the receptors activated by these kappa agonists. However, dynorphin A-(1-13) (3.2 mg/kg) did not antagonize other kappa agonists: bremazocine (0.018-0.056 mg/kg) and enadoline (0.0056-0.018 mg/kg). Taken together, these dynorphin A-(1-13) findings support the notion of functional kappa-opioid receptor subtypes, and it appears that dynorphin A-(1-13) has limited efficacy at one of these sites. Finally, dynorphin A-(1-13) (0.32 mg/kg) also antagonized the antinociceptive effects of the mu-agonist etonitazene (0.0018-0.01 mg/kg).

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Analgesics / antagonists & inhibitors
  • Analgesics / pharmacology
  • Analgesics, Opioid / pharmacology*
  • Animals
  • Anti-Arrhythmia Agents / antagonists & inhibitors
  • Anti-Arrhythmia Agents / pharmacology
  • Benzimidazoles / pharmacology
  • Benzofurans / antagonists & inhibitors
  • Benzofurans / pharmacology
  • Dynorphins / metabolism*
  • Hot Temperature
  • Macaca mulatta
  • Narcotics / pharmacology
  • Nociceptors / drug effects*
  • Pain Measurement / drug effects
  • Peptide Fragments / metabolism*
  • Pyrrolidines / antagonists & inhibitors
  • Pyrrolidines / pharmacology
  • Receptors, Opioid, kappa / agonists*
  • Receptors, Opioid, kappa / antagonists & inhibitors*

Substances

  • Analgesics
  • Analgesics, Opioid
  • Anti-Arrhythmia Agents
  • Benzimidazoles
  • Benzofurans
  • Narcotics
  • Peptide Fragments
  • Pyrrolidines
  • Receptors, Opioid, kappa
  • dynorphin (1-13)
  • Dynorphins
  • etonitazene
  • enadoline