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βARK1 inhibitor is an inhibitor of G protein-coupled receptor kinase 2/β-adrenergic receptor kinase 1 (GRK2/βARK1; IC50 = 126 μM). It is selective for GRK2/βARK1 over PKA at concentrations up to 1 mM. βARK1 inhibitor decreases systolic blood pressure in ob/ob and nicotinamide plus streptozotocin-induced mouse models of type 2 diabetes when administered at a dose of 200 μg/kg. It also improves clonidine-induced relaxation of precontracted isolated aortic rings and improves glucose tolerance in the ob/ob mouse model. βARK1 inhibitor inhibits dopamine inhibition reversal (DIR) induced by serotonin or neurotensin in the rat ventral tegmental area in vitro.

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