The individual and combined effects of U50,488, and flurbiprofen axetil on visceral pain in conscious rats.

Abstract

We examined the effects of U50,488, a kappa-opioid receptor agonist, and flurbiprofen axetil, a nonsteroidal antiinflammatory drug, in a visceral pain model using conscious rats. U50,488 produced visceral antinociception, but exaggerated the adverse effects on the central nervous system (CNS) at 0.9 mg/kg or more. Naloxone completely antagonized these effects. Flurbiprofen axetil produced visceral antinociception, but exaggerated the adverse effects on the CNS at 80 mg/kg. Coadministration of U50,488 (0.27 mg/kg) and flurbiprofen axetil (50 mg/kg) produced intense visceral antinociception without adverse effects on the CNS, implying therapeutic efficacies of coadministration of kappa-opioid receptor-agonists and nonsteroidal antiinflammatory drugs on visceral pain.

• Authors: Takayuki Kitamura, Makoto Ogawa, Yoshitsugu Yamada
• Journal: Anesthesia and analgesia (Anesth Analg) Vol. 108 Issue 6 Pg. 1964-6 (Jun 2009) ISSN: 1526-7598 [Electronic] United States
• PMID: 19448232 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Analgesics, Non-Narcotic
• Anti-Inflammatory Agents, Non-Steroidal
• Narcotic Antagonists
• Receptors, Opioid, kappa
• Flurbiprofen
• Naltrexone
• 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer
• flurbiprofen axetil

Topics

• 3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer (therapeutic use)
• Abdominal Muscles (drug effects)
• Analgesics, Non-Narcotic (therapeutic use)
• Animals
• Anti-Inflammatory Agents, Non-Steroidal (therapeutic use)
• Catheterization
• Dose-Response Relationship, Drug
• Drug Synergism
• Flurbiprofen (analogs & derivatives, therapeutic use)
• Male
• Muscle Contraction (drug effects)
• Naltrexone (pharmacology)
• Narcotic Antagonists (pharmacology)
• Pain (drug therapy)
• Pain Measurement (drug effects)
• Physical Stimulation
• Rats
• Rats, Sprague-Dawley
• Receptors, Opioid, kappa (agonists)
• Rectum (physiology)