Catalog No.S1549 Synonyms: R-65824
Molecular Weight(MW): 441.9
Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
Purity & Quality Control
Choose Selective Adrenergic Receptor Inhibitors
|Description||Nebivolol HCl selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.|
|Features||A highly cardioselective compound under certain conditions.|
Nebivolol shows high affinity and selectivity for beta 1-adrenergic receptor sites in a rabbit lung membrane preparation (Ki value = 0.9 nM and beta 2/beta 1 ratio = 50).  Nebivolol displays β1-adrenoceptor selectivity with the Ki(β2)/Ki(β1) value of 40.7 judged by competition experiments to 3H-CGP 12.1777 in the presence of CGP 207.12 A (300 nM, Kiβ2) or ICI 118.551 (50 nM, Kiβ1).  Nebivolol reduces cell proliferation of human coronary smooth muscle cells (haCSMCs) and endothelial cells (haECs) in a concentration- and time-dependent maner. Nebivolol treatment for 7 days causes significant reduction in cell growth of haCSMCs with IC50 of 6.1 μM, and inhibits accelerated haCSMC proliferation stimulated by growth factors PDGF-BB, bFGF, and TGFβ with IC50 values of 6.8 μM, 6.4 μM and 7.7 μM, repectively. Nebivolol treatment (10-5 M) of haCSMCs for 48 hours induces a moderate apoptosis of 23% and a decrease from 16% to 5% in the number of cells in S-phase. During Nebivolol incubation, NO formation of HaCEs increases, while endothelin-1 transcription and secretion are suppressed. 
|In vivo||Administratiion of Nebivolol (initially by iv within 10 minutes of reperfusion and then orally) to rats with myocardial infarction (MI) reduces myocardial apoptosis, which is mediated by regulation of NO . Nebivolol, significantly, prevents left ventricular (LV) pressure changes, reduces total and regional apoptotic cardiomyocytes. Nebivolol treatment lowers mean blood pressure (MBP) in rats with MI slightly, but not significantly. |
|In vitro||DMSO||88 mg/mL (199.14 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03655964||Recruiting||Stroke Ischemic||Aristotle University Of Thessaloniki||August 20 2018||Phase 2|
|NCT03598673||Recruiting||Hypertension||University of Abuja|Micronova Pharmaceuticals Ind Ltd||February 27 2018||--|
|NCT02619526||Recruiting||Heart Failure||Dong-A University|Menarini Group||December 2016||Not Applicable|
|NCT02467400||Active not recruiting||Osteoporosis Age-Related||Mayo Clinic||July 2015||Early Phase 1|
|NCT03245996||Completed||Aortic Blood Pressure||Tartu University Hospital||June 2015||Phase 4|
|NCT02710071||Completed||Hypertension||University of California San Diego||January 2015||Phase 4|
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