title: Nebivolol: an endothelium-friendly selective β1-adrenoceptor blocker.
abstract: 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.
authors.affiliation: Department of Physiology and Pathophysiology, Peking University, Health Science Center, Beijing, China. ygao@bjmu.edu.cn
authors.forename: Yuansheng
authors.initials: Y
authors.lastname: Gao
authors.forename: Paul M
authors.initials: PM
authors.lastname: Vanhoutte
mesh_terms: D058671:Adrenergic beta-1 Receptor Antagonists / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D000818:Animals; D001578:Benzopyrans / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D002908:Chronic Disease; D004730:Endothelium, Vascular / Q000187:drug effects* / Q000201:enzymology / Q000378:metabolism; D004983:Ethanolamines / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use*; D006333:Heart Failure / Q000188:drug therapy* / Q000378:metabolism; D006801:Humans; D006973:Hypertension / Q000188:drug therapy* / Q000378:metabolism; D015394:Molecular Structure; D000068577:Nebivolol; D009569:Nitric Oxide / Q000378:metabolism; D018384:Oxidative Stress / Q000187:drug effects; D017382:Reactive Oxygen Species / Q000378:metabolism; D014664:Vasodilation / Q000187:drug effects
chemical_list: D058671:Adrenergic beta-1 Receptor Antagonists; D001578:Benzopyrans; D004983:Ethanolamines; D017382:Reactive Oxygen Species; D000068577:Nebivolol; D009569:Nitric Oxide