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Identification and biochemical analyses of selective CB 2 agonists

, Abstract Cannabinoid CB 1 and CB 2 receptors are activated by Δ 9 -tetrahydrocannabinol, a psychoactive component of marijuana. The cannabinoid CB 1 receptor is primarily located in the brain and is responsible for the psychoactive side effects, whereas the cannabinoid CB 2 receptor is located in immune cells and is an attractive target for immune-related maladies. We identify small molecules that selectively bind to the cannabinoid CB 2 receptor and can be further developed into therapeutics. The affinity of three molecules, ABK5 , ABK6 , and ABK7 , to the cannabinoid CB 2 receptor was determined with radioligand competition binding. The potency of G-protein coupling was determined with GTP γ S binding. The three compounds bound selectively to the cannabinoid CB 2 receptor, and no binding to the cannabinoid CB 1 receptor was detected up to 10 μM. Immunoblotting studies show that the amount of ERK1/2 and MEK phosphorylation increased in a G i/o -dependent manner. Furthermore, an immune cell line (Jurkat cells) was treated with ABK5 , and as a result, inhibited cell proliferation. These three compounds are novel cannabinoid CB 2 receptor agonists and hold promise to be further developed to treat inflammation and the often-associated pain.