BQ-610

BQ-610 is a highly potent and selective ETAR (ETA receptor) antagonist (IC₅₀ = 20 nM) that ttenuates ET-induced reduction in cardiac output. It also inhibits ET-1- and ET-3-induced activation of adenylate cyclase (IC₅₀ = 28.2 nM). BQ-610 is 30-fold more potent ETA antagonist than BQ-123 in pig aortic smooth muscle membrane assay, same activity as BQ-123 when tested on pig cerebellum membrane.