The abnormal cannabidiol analogue O-1602 reduces nociception in a rat model of acute arthritis via the putative cannabinoid receptor GPR55.

Cannabinoids classically act via CB₁ and CB₂ receptors to modulate nociception; however, recent findings suggest that some cannabinoids bind to atypical receptors. One such receptor is GPR55 which is activated by the abnormal cannabidiol analogue O-1602. This study investigated whether the synthetic GPR55 agonist O-1602 can alter joint nociception in a rat model of acute joint inflammation. Acute (24 h) inflammatory joint pain was induced in male Wistar rats by intra-articular injection of 2% kaolin and 2% carrageenan. Single unit extracellular recordings were made from arthritic joint afferents in response to mechanical rotation of the knee. Peripheral administration of O-1602 significantly reduced movement-evoked firing of nociceptive C fibres and this effect was blocked by the GPR55 receptor antagonist O-1918. Co-administration of the CB₁ and CB₂ antagonists (AM281 and AM630 respectively) had no effect on O-1602 responses. This study clearly shows that atypical cannabinoid receptors are involved in joint nociception and these novel targets may be advantageous for the treatment of inflammatory pain.
AuthorsNiklas Schuelert, Jason J McDougall
JournalNeuroscience letters (Neurosci Lett) Vol. 500 Issue 1 Pg. 72-6 (Aug 1 2011) ISSN: 1872-7972 [Electronic] Ireland
PMID21683763 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
CopyrightCopyright © 2011 Elsevier Ireland Ltd. All rights reserved.
Chemical References
  • Receptor, Cannabinoid, CB1
  • Receptor, Cannabinoid, CB2
  • Receptors, G-Protein-Coupled
  • Cannabidiol
  • Kaolin
  • O-1602 compound
  • Carrageenan
  • Action Potentials
  • Acute Disease
  • Afferent Pathways
  • Animals
  • Arthritis (chemically induced, drug therapy, physiopathology)
  • Cannabidiol (analogs & derivatives, pharmacology)
  • Carrageenan
  • Hindlimb
  • Joints (drug effects, physiopathology)
  • Kaolin
  • Male
  • Movement
  • Nerve Fibers, Unmyelinated (drug effects, physiology)
  • Nociception (drug effects)
  • Rats
  • Rats, Wistar
  • Receptor, Cannabinoid, CB1 (antagonists & inhibitors)
  • Receptor, Cannabinoid, CB2 (antagonists & inhibitors)
  • Receptors, G-Protein-Coupled (agonists, antagonists & inhibitors, physiology)

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