| Popis: |
The cannabinoid CB2 receptor is one of a family of GPCRs that mediate the effects of endocannabinoids. Several agonists of this receptor are currently in clinical trials for the treatment of pain and inflammation, indications that have been validated by pre-clinical studies on agonists and in receptor knockout mice. Key to the clinical advancement of CB2 agonists is achieving selectivity over the related CB1 receptor, whose activation results in undesirable CNS effects, limiting therapeutic utility. A variety of CB2 receptor agonist chemotypes are reviewed including mono-, bi- and tricyclic cores and bi- and triaryl cores. Pharmacology, with a focus on selectivity requirements and a variety of pre-clinical animal models to assess activity and selectivity, is presented. |
