Uses
SR 59230A was used in the identification of β-adrenoceptors in rat aorta.
3 It was tested as a potential therapeutic agent in improving cardiac function in rat model of heart failure.
4
Biological Activity
Potent and selective β 3 adrenoceptor antagonist (IC 50 values are 40, 408 and 648 nM for β 3 , β 1 and β 2 receptors respectively). Orally active in vivo . Also available as part of the β -Adrenoceptor Antagonist Tocriset™ .
Biochem/physiol Actions
SR 59230A is a β3-adrenoceptor antagonist. It has high affinity for the β3 adrenoceptors occurring in human gut that affect the function of human colonic circular smooth muscle.1 It is reported that SR 59230A inhibits the Kir2.1-2.3 cardiac potassium channels.2