ArticleBritish journal of pharmacology2009
Investigation of the different adrenoceptor targets of nebivolol enantiomers in rat thoracic aorta.
Article in British journal of pharmacology, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed, 35 citations in OpenAlex.
- Effect of nebivolol on renal nitric oxide availability and tubular function in patients with essential hypertension.British journal of clinical pharmacology · 2015Trial
- Therapeutic Potential of the β3-Adrenergic Receptor and Its Ligands in Cardiovascular Diseases.International journal of molecular sciences · 2025Review
- The Endothelial Dysfunction Could Be a Cause of Heart Failure with Preserved Ejection Fraction Development in a Rat Model.Oxidative medicine and cellular longevity · 2022Article
- Effects of ambient ozone exposure on circulating extracellular vehicle microRNA levels in coronary artery disease patients.Journal of toxicology and environmental health. Part A · 2020Article
- Vasodilation Elicited by Isoxsuprine, Identified by High-Throughput Virtual Screening of Compound Libraries, Involves Activation of the NO/cGMP and H₂S/KMolecules (Basel, Switzerland) · 2019Article
- The Beta-1-Receptor Blocker Nebivolol Elicits Dilation of Cerebral Arteries by Reducing Smooth Muscle [Ca2+]i.PloS one · 2016Article
- A pathway and network review on beta-adrenoceptor signaling and beta blockers in cardiac remodeling.Heart failure reviews · 2014Review
- Effects of resveratrol and nebivolol on isolated vascular and cardiac tissues from young rats.Advances in pharmacological sciences · 2014Article
- Vasodilatory mechanisms of beta receptor blockade.Current hypertension reports · 2012Review
- Beta3-adrenoreceptor stimulation ameliorates myocardial ischemia-reperfusion injury via endothelial nitric oxide synthase and neuronal nitric oxide synthase activation.Journal of the American College of Cardiology · 2011Article
- Beta-3 adrenoceptors as new therapeutic targets for cardiovascular pathologies.Current heart failure reports · 2011Review
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Authors and funding
4 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
background and purposeNebivolol is a highly selective beta(1)-adrenoceptor antagonist with beta(3)-adrenoceptor agonist properties and is a racemate mixture of D- and L-enantiomers. However, the cellular mechanisms of the effects of each enantiomer are not yet clear and are a matter for debate. The aim of the present experiments was to determine the adrenoceptors involved in the vascular effects of D- and L-enantiomers of nebivolol in rat thoracic aorta. EXPERIMENTAL APPROACH: Responses to nebivolol enantiomers were evaluated in rings of thoracic aorta from male Sprague-Dawley rats. KEY
resultsD-nebivolol (0.1-10 micromol.L(-1)), but not L-nebivolol, significantly shifted to the right the concentration-response curve to phenylephrine, an alpha(1)-adrenoceptor agonist, in a concentration-dependent manner. For the following experiments, aortic rings were constricted with endothelin 1 and now both enantiomers produced an endothelium-dependent relaxation of the rings involving the nitric oxide pathway. This relaxation was not modified by 1 micromol.L(-1) CGP 20,712A (beta(1)-adrenoceptor antagonist), but significantly blunted by 7 micromol.L(-1) L-74,8337 (beta(3)-adrenoceptor antagonist). However, only the vasorelaxation induced by D-nebivolol was significantly reduced by 1 micromol.L(-1) ICI 118,551 (beta(2)-adrenoceptor antagonist). CONCLUSIONS AND IMPLICATIONS: Our results suggest that the nebivolol enantiomers act on different targets. D-nebivolol induced vasorelaxation by activating beta(2)- and beta(3)-adrenoceptors and antagonizing alpha(1)-adrenoceptors. L-nebivolol induced vasorelaxation by activating only beta(3)-adrenoceptors in our model. Our results emphasize that nebivolol is a beta(1)-adrenoceptor antagonist with several important pharmacological differences from other beta(1)-adrenoceptor antagonists.
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