Nebivolol is a third generation β1 selective beta-blocker with vasodilatory properties which is approved for the treatment of hypertension and heart failure. The vasodilatory effect is nitric-oxide mediated and activated via β3-agonism. Nebivolol has the highest β1-receptor affinity among β-blockers and it substantially improves endothelial dysfunction by its strong stimulatory effects on the activity of the endothelial NOS and via its antioxidative properties. Nebivolol reverses endothelial dysfunction in animal models of oxidative stress and human studies. In vitro, nebivolol has been shown to inhibit platelet aggregation and has antiproliferative effects.