ArticleBritish journal of pharmacology2006
Mixed beta3-adrenoceptor agonist and alpha1-adrenoceptor antagonist properties of nebivolol in rat thoracic aorta.
Article in British journal of pharmacology, 2006. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.
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Who cites it
17 citing papers in PubMed, 60 citations in OpenAlex.
- Biased Agonism at β-Adrenoceptor Subtypes: A Drug Development Perspective.Handbook of experimental pharmacology · 2026Review
- Role of β-Adrenergic Receptors in Stress-Induced Cardiac Injury.Bulletin of experimental biology and medicine · 2025Article
- Role and mechanism of miRNA in cardiac microvascular endothelial cells in cardiovascular diseases.Frontiers in cardiovascular medicine · 2024Review
- Role of endothelial dysfunction in heart failure.Heart failure reviews · 2020Review
- Rationale for nebivolol/valsartan combination for hypertension: review of preclinical and clinical data.Journal of hypertension · 2017Review
- Role of βInternational journal of clinical and experimental pathology · 2017Article
- Mirabegron relaxes urethral smooth muscle by a dual mechanism involving β3 -adrenoceptor activation and α1 -adrenoceptor blockade.British journal of pharmacology · 2016Article
- β3-adrenoceptor impacts apoptosis in cultured cardiomyocytes via activation of PI3K/Akt and p38MAPK.Journal of Huazhong University of Science and Technology. Medical sciences = Hua zhong ke ji da xue xue bao. Yi xue Ying De wen ban = Huazhong keji daxue xuebao. Yixue Yingdewen ban · 2016Article
- β1-Adrenergic receptor blockade extends the life span of Drosophila and long-lived mice.Age (Dordrecht, Netherlands) · 2013Article
- New advances in beta-blocker therapy in heart failure.Frontiers in physiology · 2013Review
- Vasodilatory mechanisms of beta receptor blockade.Current hypertension reports · 2012Review
- Clinical and economic aspects of the use of nebivolol in the treatment of elderly patients with heart failure.Clinical interventions in aging · 2010Review
- Ligand-directed signalling at beta-adrenoceptors.British journal of pharmacology · 2010Review
- Investigation of the different adrenoceptor targets of nebivolol enantiomers in rat thoracic aorta.British journal of pharmacology · 2009Article
- Blood pressure-lowering effect of nebivolol in hypertensive patients with type 2 diabetes mellitus: the YESTONO study.Clinical drug investigation · 2007Article
- New drugs for hypertension: what do they offer?Current hypertension reports · 2006Review
- Hypoglycemia, polycythemia and hyponatremia in a newborn exposed to nebivolol during pregnancy.Journal of pharmacology & pharmacotherapeuticsArticle
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nebivolol, a selective beta-adrenoceptor (beta1-AR) antagonist, induces vasodilatation by an endothelium- and NO-cGMP-dependent pathway. However, the mechanisms involved in the vascular effect of nebivolol have not been established. Thus, we evaluated the role of alpha1 and beta3-ARs in nebivolol-induced vasodilatation. The responses to nebivolol were investigated in vitro in thoracic aortic rings isolated from male Sprague-Dawley rats. Nebivolol (0.1-10 microM) significantly shifted the concentration-response curve to phenylephrine, an alpha1-AR agonist, to the right in a concentration-dependent manner (pA2 = 6.5). Conversely, the concentration-response curve to endothelin 1 (ET1) was unaffected by nebivolol. In ET1-precontracted rings, nebivolol induced a concentration-dependent relaxation, which was unaffected by nadolol (a beta1/beta2-AR antagonist) but was significantly reduced by L-748,337 (a beta3-AR antagonist), endothelium removal or pretreatment with L-NMMA (an NOS inhibitor). Similar results were obtained with a beta3-AR agonist, SR 58611A. It was concluded that, in rat aorta, nebivolol-induced relaxation results from both inhibition of alpha1-ARs and activation of beta3-ARs. In addition, we confirmed that the endothelium and the NO pathway are involved in the vascular effect of nebivolol. The identification of these vascular targets of nebivolol indicate that it has therapeutic potential for the treatment of pathological conditions associated with an elevation of sympathetic tone, such as heart failure and hypertension.
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