1135278-41-9

SR 59230A (hydrochloride) is a β₃-adrenergic receptor (β₃-AR) antagonist (pA₂s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively). It is less selective for β₃-AR in cells transfected with the human β-AR subtypes (K_is = 16.4, 61.9, and 122 nM for β₁-, β₂-, and β₃-AR, respectively). At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α₁-AR antagonistic mechanism. In adipocytes, it induces phosphorylation of p38 MAPK via the G_s pathway. It has also been used in studies of heart failure to elucidate the role of the β₃-ARs.

SR 59230A Hydrochloride is a potent and selective β3 adrenergic receptor antagonist.

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