Nitric oxide mechanisms of nebivolol

Research output: Contribution to journalArticle

Abstract

β-blockers are among the most widely used drugs in the prevention and treatment of cardiovascular disease, although they are associated with increased peripheral resistance. Third-generation β-blockers avoid this adverse effect by inducing vasodilation through different mechanisms. In particular, nebivolol, a highly selective blocker of β1-adrenergic receptors, is the only β-blocker known to induce vascular production of nitric oxide, the main endothelial vasodilator. The specific mechanism of nebivolol is particularly relevant in hypertension, where nitric oxide dysfunction occurs. Indeed, nebivolol is able to reverse endothelial dysfunction. Nebivolol induces nitric oxide production via activation of β3-adrenergic receptors, which can explain the good metabolic profile observed after treatment with this drug. Moreover, nebivolol can also stimulate the β3-adrenergic receptor-mediated production of nitric oxide in the heart, and this stimulation can result in a greater protection against heart failure. In conclusion, nebivolol has a unique profile among antihypertensive drugs, adding to a very high selectivity against β1 adrenergic receptors, and an agonist action on β3 receptors and nitric oxide (NO), which has led to clinically significant improvements in hypertensive patients.

Original languageEnglish
Pages (from-to)317-327
Number of pages11
JournalTherapeutic Advances in Cardiovascular Disease
Volume3
Issue number4
DOIs
Publication statusPublished - 2009

Keywords

  • Beta1-adrenergic receptors
  • Beta3-adrenergic receptors
  • Heart
  • Nebivolol
  • Nitric oxide
  • Vessels

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine
  • Pharmacology (medical)

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