Carvedilol is a non-selective β-antagonist with α1-adrenolytic activity that binds the α1-, α2-, and β1-adrenoceptors with Ki values of 2.2 nM, 3.4 μM, and 0.81 nM, respectively. By inhibiting excess stimulation of catecholamine it demonstrates antiarrhythmic activity in a rat model of adrenaline-induced arrhythmia with an ED50 value of 0.25 mg/kg. Carvedilol has also been shown to activate cardioprotective signaling through β-arrestin and ERK1/2 activation (EC50 = 2 nM).
