An inhibitor of GRK2/βARK1 (IC50 = 126 μM); selective for GRK2/βARK1 over PKA at concentrations up to 1 mM; decreases systolic blood pressure in ob/ob and nicotinamide plus streptozotocin-induced mouse models of type 2 diabetes at 200 μg/kg; improves clonidine-induced relaxation of precontracted isolated aortic rings and improves glucose tolerance in the ob/ob mouse model; inhibits serotonin- or neurotensin-induced DIR in the rat ventral tegmental area in vitro