Cannabinoid CB2 receptor agonist activity in the hindpaw incision model of postoperative pain

Eur J Pharmacol. 2005 Dec 19;527(1-3):172-4. doi: 10.1016/j.ejphar.2005.10.020. Epub 2005 Nov 28.

Abstract

The identification of peripherally expressed CB2 receptors and reports that the selective activation of cannabinoid CB2 receptors produces antinociception without traditional cannabinergic side effects suggests that selective cannabinoid CB2 receptor agonists might be useful in the management of pain. In a rat hindpaw incision model, we examined the antiallodynic activity of the selective cannabinoid CB2 receptor agonists AM1241 (3-30 mg/kg i.p.), GW405833 (3-30 mg/kg i.p.), and HU-308 (0.3-30 mg/kg i.p.). The rank order for efficacy in the hindpaw incision model following a dose of 10 mg/kg, i.p. was AM1241 > GW405833 = HU-308, and the selective cannabinoid CB2 receptor antagonist, SR144528, reversed the antiallodynic effect of HU-308. Together, these data suggest that selective cannabinoid CB2 receptor agonists might represent a new class of postoperative analgesics.

MeSH terms

  • Animals
  • Camphanes / administration & dosage
  • Camphanes / therapeutic use
  • Cannabinoids / administration & dosage
  • Cannabinoids / therapeutic use
  • Drug Administration Schedule
  • Foot Injuries / surgery
  • Hindlimb / surgery*
  • Indoles / administration & dosage
  • Indoles / therapeutic use
  • Male
  • Models, Animal
  • Morpholines / administration & dosage
  • Morpholines / therapeutic use
  • Pain / prevention & control
  • Pain Measurement / methods
  • Pain, Postoperative / physiopathology
  • Pain, Postoperative / prevention & control*
  • Pyrazoles / administration & dosage
  • Pyrazoles / therapeutic use
  • Rats
  • Rats, Sprague-Dawley
  • Receptor, Cannabinoid, CB2 / agonists*
  • Receptor, Cannabinoid, CB2 / antagonists & inhibitors
  • Time Factors

Substances

  • 1-(2,3-dichlorobenzoyl)-5-methoxy-2-methyl-(2-(mopholin-4-yl)ethyl)-1H-indole
  • AM 1241
  • Camphanes
  • Cannabinoids
  • Indoles
  • Morpholines
  • Pyrazoles
  • Receptor, Cannabinoid, CB2
  • SR 144528
  • HU 308