Additive antinociceptive effects of mixtures of the κ-opioid receptor agonist spiradoline and the cannabinoid receptor agonist CP55940 in rats

Behav Pharmacol. 2016 Feb;27(1):69-72. doi: 10.1097/FBP.0000000000000184.

Abstract

Pain is a significant clinical problem, and there is a need for pharmacotherapies that are more effective with fewer adverse effects than currently available medications. Cannabinoid receptor agonists enhance the antinociceptive effects of μ-opioid receptor agonists; it is unclear whether they impact the effects of agonists acting at other opioid receptors. κ-Opioid receptor agonists have antinociceptive effects, but their clinical use is precluded by adverse effects; however, their therapeutic potential might be realized if antinociceptive effects could be selectively enhanced. In this study, the antinociceptive effects of the cannabinoid receptor agonist CP55940 and the κ-opioid receptor agonist spiradoline, alone and in combination, were studied in rats (n=7) using a warm water tail-withdrawal procedure. When administered alone, CP55940 (0.032-1.0 mg/kg) and spiradoline (1.0-32.0 mg/kg) increased tail-withdrawal latency, and mixtures of CP55940 and spiradoline (ratios of 1 : 3, 1 : 1, and 3 : 1) produced additive effects. It remains to be determined whether this additive interaction between a κ-opioid receptor agonist and a cannabinoid receptor agonist is selective for antinociception and whether it can be generalized to other drugs.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Analgesics / pharmacology*
  • Animals
  • Cannabinoid Receptor Agonists / pharmacology*
  • Cyclohexanols / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Therapy, Combination
  • Hot Temperature
  • Male
  • Nociceptive Pain / drug therapy*
  • Pain Threshold / drug effects
  • Pyrrolidines / pharmacology*
  • Rats, Sprague-Dawley
  • Receptors, Opioid, kappa / agonists*

Substances

  • Analgesics
  • Cannabinoid Receptor Agonists
  • Cyclohexanols
  • Pyrrolidines
  • Receptors, Opioid, kappa
  • 3-(2-hydroxy-4-(1,1-dimethylheptyl)phenyl)-4-(3-hydroxypropyl)cyclohexanol
  • spiradoline