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Nebivolol

Names

[ CAS No. ]:
118457-14-0

[ Name ]:
Nebivolol

[Synonym ]:
Dexnebivolol
Nobiten
l-nebivolol
dl-Nebivolol
(1R)-1-[(2R)-6-Fluoro-3,4-dihydro-2H-chromen-2-yl]-2-({(2R)-2-[(2S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]-2-hydroxyethyl}amino)ethanol
(1R,1'R)-2,2'-iminobis{1-[(2R,2'S)-6-fluoro-3,4-dihydro-2H-chromen-2-yl]ethanol}
Vasoxen
2H-1-Benzopyran-2-methanol, α,α'-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-, (αR,2S)-
UNII:030Y90569U
(S,R,R,R)-nebivolol
Levonebivolol
Nebivolol

Biological Activity

[Description]:

Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM.Target: β1- adrenergic receptorNebivolol 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.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Cardiovascular Disease

[References]

[1]. Brehm BR, et al. Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cells. Cardiovasc Res. 2001 Feb 1;49(2):430-9.

[2]. Mercanoglu G, et al. The effects of nebivolol on apoptosis in a rat infarct model. Circ J. 2008 Apr;72(4):660-70.


[Related Small Molecules]

Isoprenaline hydrochloride | ICI 118,551 (hydrochloride) | Phenylephrine hydrochloride | Yohimbine hydrochloride | Adrenaline | Ivabradine hydrochloride | Prazosin hydrochloride | Clenbuterol hydrochloride | Phentolamine mesilate | guanfacine hydrochloride | pimozide | Sotalol hydrochloride | Carvedilol | Atenolol | Metroprolol succinate

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
600.5±55.0 °C at 760 mmHg

[ Molecular Formula ]:
C22H25F2NO4

[ Molecular Weight ]:
405.435

[ Flash Point ]:
316.9±31.5 °C

[ Exact Mass ]:
405.175171

[ PSA ]:
100.62000

[ LogP ]:
3.67

[ Vapour Pressure ]:
0.0±1.8 mmHg at 25°C

[ Index of Refraction ]:
1.581

[ Storage condition ]:
-20℃

Related Compounds