title: Should peripheral CB(1) cannabinoid receptors be selectively targeted for therapeutic gain?
abstract: Endocannabinoids, endogenous lipid ligands of cannabinoid receptors, mediate a variety of effects similar to those of marijuana. Cannabinoid CB(1) receptors are highly abundant in the brain and mediate psychotropic effects, which limits their value as a potential therapeutic target. There is growing evidence for CB(1) receptors in peripheral tissues that modulate a variety of functions, including pain sensitivity and obesity-related hormonal and metabolic abnormalities. In this review we propose that selective targeting of peripheral CB(1) receptors has potential therapeutic value because it would help to minimize addictive, psychoactive effects in the case of CB(1) agonists used as analgesics, or depression and anxiety in the case of CB(1) antagonists used in the management of cardiometabolic risk factors associated with the metabolic syndrome.
authors.affiliation: Laboratory of Physiologic Studies, National Institute on Alcohol Abuse and Alcoholism, Bethesda, MD 20892, USA. gkunos@mail.nih.gov
authors.forename: George
authors.initials: G
authors.lastname: Kunos
authors.forename: Douglas
authors.initials: D
authors.lastname: Osei-Hyiaman
authors.forename: Sándor
authors.initials: S
authors.lastname: Bátkai
authors.forename: Keith A
authors.initials: KA
authors.lastname: Sharkey
authors.forename: Alexandros
authors.initials: A
authors.lastname: Makriyannis
mesh_terms: D000818:Animals; D015195:Drug Design; D006801:Humans; D007249:Inflammation / Q000503:physiopathology / Q000517:prevention & control; D008659:Metabolic Diseases / Q000188:drug therapy* / Q000503:physiopathology / Q000517:prevention & control; D010146:Pain / Q000188:drug therapy / Q000503:physiopathology / Q000517:prevention & control; D043884:Receptor, Cannabinoid, CB1 / Q000037:antagonists & inhibitors* / Q000502:physiology; D009626:Terminology as Topic
chemical_list: D043884:Receptor, Cannabinoid, CB1