CB2 cannabinoid receptor agonists: pain relief without psychoactive effects?
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.
Malan
T Philip
TP
Department of Anaesthesiology, The University of Arizona, Tucson, AZ 85724, USA.
Ibrahim
Mohab M
MM
Lai
Josephine
J
Vanderah
Todd W
TW
Makriyannis
Alexandros
A
Porreca
Frank
F
D000700:Analgesics / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D002186:Cannabinoids / Q000494:pharmacology / Q000627:therapeutic use*; D006801:Humans; D010146:Pain / Q000188:drug therapy* / Q000378:metabolism; D011619:Psychotropic Drugs / Q000494:pharmacology / Q000627:therapeutic use*; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug / Q000819:agonists* / Q000378:metabolism
D000700:Analgesics; D002186:Cannabinoids; D011619:Psychotropic Drugs; D043882:Receptors, Cannabinoid; D011955:Receptors, Drug