Nebivolol is a highly selective β1-adrenoceptor blocker, which also stimulates endothelial nitric oxide synthase and scavenges reactive oxygen species (ROS). These characteristics endow nebivolol, compared with conventional β-blockers, with a favorable hemodynamic profile for the treatment of hypertension, chronic heart failure, and possibly other cardiovascular diseases. Nebivolol is a racemic mixture of d- and l-isomers. Its β1-antagonistic properties reside primarily with d-nebivolol although both isomers are capable of increasing the release of NO from the endothelium after binding to β2- or β3-adrenergic receptors. The latter action results in vasodilatation and reduced vascular resistance. Nebivolol also scavenges ROS in a receptor-independent manner by direct interaction with free radicals. By scavenging ROS nebivolol not only reduces oxidant stress but also augments NO bioavailability. The endothelial nitric oxide synthase -stimulating and ROS scavenging effects of nebivolol act synergistically to provide cardiovascular protection in addition to its β1-antagonistic action.