Dose-independent antinociceptive interaction of endogenous ligands at the spinal level

Brain Res. 2004 Dec 10;1029(1):93-102. doi: 10.1016/j.brainres.2004.09.039.

Abstract

Adenosine, agmatine and kynurenic acid are endogenous ligands acting on different (e.g. adenosine, NMDA, alpha(2)-adrenergic and imidazoline) receptors with a potential role in nociception at the spinal level. Their antinociceptive effects have already been investigated as monotherapy, but only a few studies have reported on their effects on the potency of other drugs. The purpose of the present study was carried out to analyse their interactions during continuous intrathecal co-administration in a carrageenan-induced thermal hyperalgesia model in rats. A paw withdrawal test was used for nociceptive testing. The intrathecal infusion (60 min) of these three drugs was administered alone or in combinations (kynurenic acid+adenosine or agmatine; adenosine+agmatine), which was followed by an additional 60-min observation period. Kynurenic acid alone was ineffective, while adenosine and agmatine alone caused a slight increase in pain threshold. However, independently of the applied doses all of the combinations significantly (p<0.05) increased the paw withdrawal latencies on the inflamed side during and after the infusion, but were almost ineffective on the normal side. The adenosine+kynurenic acid combination was the most effective: namely, that it relieved thermal hyperalgesia in all the applied dose combinations. Treatment with the kynurenic acid-containing combinations also caused dose-dependent side-effects (motor impairment and excitation), despite the fact that monotherapy with kynurenic acid in the applied dose (0.1 microg/min) did not result in adverse effects.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine / administration & dosage*
  • Agmatine / administration & dosage*
  • Analgesics / administration & dosage*
  • Animals
  • Carrageenan
  • Dose-Response Relationship, Drug
  • Drug Combinations
  • Drug Synergism
  • Excitatory Amino Acid Antagonists / administration & dosage
  • Hyperalgesia / chemically induced
  • Injections, Spinal
  • Kynurenic Acid / administration & dosage*
  • Ligands
  • Male
  • Pain Threshold / drug effects*
  • Rats
  • Rats, Wistar
  • Reaction Time / drug effects

Substances

  • Analgesics
  • Drug Combinations
  • Excitatory Amino Acid Antagonists
  • Ligands
  • Agmatine
  • Carrageenan
  • Kynurenic Acid
  • Adenosine