Enadoline discrimination in squirrel monkeys: effects of opioid agonists and antagonists

J Pharmacol Exp Ther. 2001 Apr;297(1):215-23.

Abstract

Squirrel monkeys were trained to discriminate i.m. injections of the kappa-opioid receptor agonist enadoline (0.0017 mg/kg) from saline in a two-lever drug-discrimination procedure. Enadoline produced a reliable discriminative stimulus that was reproduced by the kappa-selective agonists PD 117302, U 50,488, GR 89686A, (-)-spiradoline, ICI 204448, and EMD 61753, and by the mixed-action kappa/mu-agonists bremazocine and ethylketocyclazocine. The discriminative stimulus effects of enadoline were not reproduced by the mu-selective agonist morphine, the delta-selective agonist BW373U86, the mixed-action opioids nalbuphine and nalorphine, or by the less active enantiomers of enadoline and spiradoline PD 129829 and (+)-spiradoline, respectively. The selective mu-opioid antagonist beta-funaltrexamine (10.0 mg/kg) did not appreciably alter the dose-effect function for enadoline in any subject. However, the nonselective and kappa-selective opioid antagonists quadazocine (0.03-3.0 mg/kg) and nor-BNI (3-10 mg/kg), and the mixed-action opioid nalbuphine (0.3-30 mg/kg) served to surmountably antagonize enadoline's discriminative stimulus effects. The antagonist effects of nor-BNI were long-lasting and did not distinguish between drugs purported to act at different kappa-receptor subtypes. The present results bolster the view that common discriminative stimulus effects of enadoline and other opioids are mediated by kappa-agonist actions that are surmountably antagonized by nor-BNI in a long-lasting manner. The enadoline-antagonist effects of nalbuphine support the idea that it acts with low efficacy at kappa-opioid receptors.

Publication types

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

MeSH terms

  • Animals
  • Benzofurans / pharmacology*
  • Discrimination Learning / drug effects*
  • Dose-Response Relationship, Drug
  • Male
  • Nalbuphine / pharmacology
  • Naltrexone / analogs & derivatives
  • Naltrexone / pharmacology
  • Narcotic Antagonists / pharmacology*
  • Pyrroles / pharmacology
  • Pyrrolidines / pharmacology*
  • Receptors, Opioid, kappa / agonists*
  • Receptors, Opioid, kappa / physiology
  • Receptors, Opioid, mu / physiology
  • Saimiri
  • Thiophenes / pharmacology

Substances

  • Benzofurans
  • Narcotic Antagonists
  • Pyrroles
  • Pyrrolidines
  • Receptors, Opioid, kappa
  • Receptors, Opioid, mu
  • Thiophenes
  • PD 117302
  • norbinaltorphimine
  • Naltrexone
  • beta-funaltrexamine
  • enadoline
  • Nalbuphine