SR 144528 is a selective peripheral CB2 (cannabinoid) receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors. SR 144528 antagonizes the inhibitory effects of CP 55,940 on forskolin-induced adenylyl cyclase activity in CHO cells expressing hCB2. SR 144528 has also been used to investigate the contribution of the CB2 receptor in the control of pain initiation as well as suppression of inflammation and immune activation.
