CB2 cannabinoid receptor agonists: pain relief without psychoactive effects?

Curr Opin Pharmacol. 2003 Feb;3(1):62-7. doi: 10.1016/s1471-4892(02)00004-8.


Cannabinoid receptor agonists significantly diminish pain responses in animal models; however, they exhibit only modest analgesic effects in humans. The relative lack of efficacy in man may be because of the dose limitations imposed by psychoactive side effects. Cannabinoid agonists that selectively target CB(2) (peripheral) cannabinoid receptors should be free of psychoactive effects, perhaps allowing for more effective dosing. CB(2) receptor activation inhibits acute, inflammatory and neuropathic pain responses in animal models. In preclinical studies, CB(2) receptor agonists do not produce central nervous system effects. Therefore, they show promise for the treatment of acute and chronic pain without psychoactive effects.

Publication types

  • Research Support, U.S. Gov't, P.H.S.
  • Review

MeSH terms

  • Analgesics / pharmacology
  • Analgesics / therapeutic use
  • Animals
  • Cannabinoids / pharmacology
  • Cannabinoids / therapeutic use*
  • Humans
  • Pain / drug therapy*
  • Pain / metabolism
  • Psychotropic Drugs / pharmacology
  • Psychotropic Drugs / therapeutic use*
  • Receptors, Cannabinoid
  • Receptors, Drug / agonists*
  • Receptors, Drug / metabolism


  • Analgesics
  • Cannabinoids
  • Psychotropic Drugs
  • Receptors, Cannabinoid
  • Receptors, Drug