TherapeuticUtility of Cannabinoid Receptor Type 2 (CB2) SelectiveAgonists.

Thecannabinoid receptor type 2 (CB2) is a class A GPCR thatwas cloned in 1993 while looking for an alternative receptor thatcould explain the pharmacological properties of Δ9-tetrahydrocannabinol. CB2was identified among cDNAsbased on its similarity in amino acid sequence to the CB1receptor and helped provide an explanation for the established effectsof cannabinoids on the immune system. In addition to the immune system,CB2has widespread tissue expression and has been foundin brain, peripheral nervous system, and gastrointestinal tract. Several“mixed” cannabinoid agonists are currently in clinicaluse primarily for controlling pain, and it is believed that selectiveCB2agonism may afford a superior analgesic agent devoidof the centrally mediated CB1effects. Thus, selectiveCB2receptor agonists represent high value putative therapeuticsfor treating pain and other disease states. In this Perspective, weseek to provide a concise update of progress in the field. [ABSTRACT FROM AUTHOR]