SR 144528 is a selective peripheral cannabinoid (CB2) 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 (IC50 = 10 nM) but not in cells expressing hCB1 (IC50 > 10 uM). SR 144528 has 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.
产品描述
A selective CB2 receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors (Ki = 400 nM for rat brain and human CB1 receptors)