Description
SR 59230A (hydrochloride) is a β
3-adrenergic receptor (β
3-AR) antagonist (pA
2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively). It is less selective for β
3-AR in cells transfected with the human β-AR subtypes (K
is = 16.4, 61.9, and 122 nM for β
1-, β
2-, and β
3-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 α
1-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 β
3-ARs.
