Modulation of paracetamol antinociception by caffeine and by selective adenosine A2 receptor antagonists in mice

Eur J Pharmacol. 2006 Feb 15;531(1-3):80-6. doi: 10.1016/j.ejphar.2005.12.004. Epub 2006 Jan 30.

Abstract

This study investigated the involvement of adenosine receptors in the interaction between paracetamol and caffeine in mice, using the adenosine A2A receptor antagonist 5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine (SCH58261) and the adenosine A2B receptor antagonist 1-propyl-8-p-sulfophenylxanthine (PSB1115), in the tail immersion and hot-plate tests. Paracetamol (10-200 mg/kg) was antinociceptive in both tests, but, in contrast to previous studies, caffeine (10 mg/kg) was pronociceptive in the tail immersion test, and reduced the effects of paracetamol in both tests. SCH58261 (3 mg/kg) was antinociceptive in both tests and in its presence paracetamol (50 mg/kg) had no further effect. PSB1115 (10 mg/kg) had little effect alone but potentiated the effect of paracetamol (50 mg/kg) in the hot-plate test and abolished it in the tail immersion test. These results suggest that adenosine A2B receptors may be involved in the action of paracetamol in a pathway-dependent manner, and also support the existence of pronociceptive adenosine A2A receptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetaminophen / pharmacology*
  • Adenosine A2 Receptor Antagonists*
  • Analgesics, Non-Narcotic / pharmacology
  • Animals
  • Caffeine / pharmacology*
  • Central Nervous System Stimulants / pharmacology
  • Dose-Response Relationship, Drug
  • Female
  • Male
  • Mice
  • Mice, Knockout
  • Neuroprotective Agents / pharmacology
  • Nociceptors / drug effects*
  • Nociceptors / physiopathology
  • Pain / physiopathology
  • Pain / prevention & control
  • Pain Measurement / methods
  • Pyrimidines / pharmacology*
  • Receptor, Adenosine A2A / genetics
  • Receptor, Adenosine A2A / physiology
  • Receptor, Adenosine A2B / physiology
  • Sulfonic Acids / pharmacology
  • Time Factors
  • Triazoles / pharmacology*
  • Xanthines / pharmacology

Substances

  • 5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo(4,3-e)-1,2,4-triazolo(1,5-c)pyrimidine
  • Adenosine A2 Receptor Antagonists
  • Analgesics, Non-Narcotic
  • Central Nervous System Stimulants
  • Neuroprotective Agents
  • Pyrimidines
  • Receptor, Adenosine A2A
  • Receptor, Adenosine A2B
  • Sulfonic Acids
  • Triazoles
  • Xanthines
  • Acetaminophen
  • Caffeine