Targeting cannabinoid agonists for inflammatory and neuropathic pain

Expert Opin Investig Drugs. 2007 Jul;16(7):951-65. doi: 10.1517/13543784.16.7.951.


The cannabinoid receptors CB(1) and CB(2) are class A G-protein-coupled receptors. It is well known that cannabinoid receptor agonists produce relief of pain in a variety of animal models by interacting with cannabinoid receptors. CB(1) receptors are located centrally and peripherally, whereas CB(2) receptors are expressed primarily on immune cells and tissues. A large body of preclinical data supports the hypothesis that either CB(2)-selective agonists or CB(1) agonists acting at peripheral sites, or with limited CNS exposure, will inhibit pain and neuroinflammation without side effects within the CNS. There has been a growing interest in developing cannabinoid agonists. Many new cannabinoid ligands have been synthesized and studied covering a wide variety of novel structural scaffolds. This review focuses on the present development of cannabinoid agonists with an emphasis on selective CB(2) agonists and peripherally restricted CB(1) or CB(1)/CB(2) dual agonists for treatment of inflammatory and neuropathic pain.

Publication types

  • Review

MeSH terms

  • Analgesics / pharmacology
  • Analgesics / therapeutic use
  • Animals
  • Cannabinoids / pharmacology
  • Cannabinoids / therapeutic use*
  • Disease Models, Animal
  • Drugs, Investigational*
  • Humans
  • Inflammation / diagnosis
  • Inflammation / drug therapy
  • Neuralgia / diagnosis
  • Neuralgia / drug therapy*
  • Neuritis / diagnosis
  • Neuritis / drug therapy
  • Pain Measurement
  • Pain, Intractable / diagnosis
  • Pain, Intractable / drug therapy*
  • Prospective Studies
  • Rats
  • Receptor, Cannabinoid, CB2 / drug effects*
  • Receptors, Drug / agonists
  • Receptors, Drug / antagonists & inhibitors
  • Receptors, Drug / metabolism
  • Risk Assessment
  • Sensitivity and Specificity


  • Analgesics
  • Cannabinoids
  • Drugs, Investigational
  • Receptor, Cannabinoid, CB2
  • Receptors, Drug