Alprenolol is a non-selective β-antagonist that binds β1-, β2-, and β3-adrenoceptors with Ki values of 5.8, 1.2, and 35 nM, respectively. It crosses the blood brain barrier and antagonizes serotonin 5HT1A receptors. Alprenolol has been shown to activate cardioprotective signaling through β-arrestin and ERK1/2 activation (EC50 = 59 nM).
