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HERO ID
875345
Reference Type
Journal Article
Subtype
Review
Title
Nebivolol: An Endothelium-Friendly Selective β1-Adrenoceptor Blocker
Author(s)
Gao, Y; Vanhoutte, PM
Year
2012
Is Peer Reviewed?
Yes
Journal
Journal of Cardiovascular Pharmacology
ISSN:
0160-2446
EISSN:
1533-4023
Volume
59
Issue
1
Page Numbers
16-21
Language
English
PMID
21283024
DOI
10.1097/FJC.0b013e3182073e27
Web of Science Id
WOS:000298669500003
Abstract
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.
Keywords
nitric oxide; beta-blocker; reactive oxygen species; hypertension; chronic heart failure
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