Updating the chemistry and biology of cannabinoid CB2 receptor-specific inverse agonists.
The cannabinoid CB(2) receptor continues to be an intriguing target for the potential therapeutic benefit of cannabinoids. Because this receptor is significantly found outside the brain, compounds specific for the CB(2) receptor may be free of the side effects that have plagued cannabinoid CB(1) receptor-based therapeutics. In this review, we will discuss a class of compounds which modulate the constitutive activity of the cannabinoid CB(2) receptor, the inverse agonists. We will discuss recent chemical advances that provide new compounds to investigate the biology based on this pharmacology. We will then discuss new biology associated with the cannabinoid CB(2) receptor for hints of how these compounds can best be utilized in vivo.
Lunn
Charles A
CA
New Lead Discovery / Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, New Jersey, USA. charles.lunn@spcorp.com
D000818:Animals; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002185:Cannabidiol / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use; D002186:Cannabinoids / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D002465:Cell Movement / Q000187:drug effects / Q000502:physiology; D054314:Drug Inverse Agonism; D006801:Humans; D007249:Inflammation / Q000188:drug therapy / Q000473:pathology; D043885:Receptor, Cannabinoid, CB2 / Q000819:agonists* / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism
D002186:Cannabinoids; D043885:Receptor, Cannabinoid, CB2; D002185:Cannabidiol