Health & Environmental Research Online (HERO)


Print Feedback Export to File
875345 
Journal Article 
Review 
Nebivolol: An Endothelium-Friendly Selective β1-Adrenoceptor Blocker 
Gao, Y; Vanhoutte, PM 
2012 
Yes 
Journal of Cardiovascular Pharmacology
ISSN: 0160-2446
EISSN: 1533-4023 
59 
16-21 
English 
Nebivolol is a highly selective β1-adrenoceptor (AR) blocker which also stimulates endothelial nitric oxide synthase (eNOS) and scavenges reactive oxygen species (ROS). These characteristics endow nebivolol, compared to 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 while both isomers are capable of increasing the release of nitric oxide (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 eNOS stimulating and ROS scavenging effects of nebivolol act synergistically to provide cardiovascular protection in addition to its β1-antagonistic action. 
nitric oxide; beta-blocker; reactive oxygen species; hypertension; chronic heart failure