Nebivolol hydrochloride (R-65824)
For research use only.
CAS No. 152520-56-4
Nebivolol HCl (R-65824) selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM.
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|Description||Nebivolol HCl (R-65824) 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. 
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||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01885988||Unknown status||Drug: Nebivolol|Drug: Sugar Pill||Erectile Dysfunction||Martin M. Miner MD|Forest Laboratories|The Miriam Hospital||March 2013||Phase 4|
|NCT01057251||Completed||Drug: Nebivolol|Drug: Placebo||Hypertension||Forest Laboratories||March 2010||Phase 4|
|NCT01077661||Completed||Drug: Nebivolol||Hypertension|Heart Failure||GlaxoSmithKline||October 2009||--|
|NCT00999752||Completed||Drug: Nebivolol|Drug: Hydrochlorothiazide||Hypertension||InVasc Therapeutics Inc.||October 2009||Not Applicable|
|NCT00683124||Unknown status||Drug: Losartan and nebivolol|Drug: Losartan|Drug: Nebivolol||Marfan Syndrome||IRCCS Policlinico S. Matteo|Merck Sharp & Dohme Corp.|Menarini Group||July 2008||Phase 3|
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