Nebivolol

Names

[ Name ]:
Nebivolol

[Synonym ]:
Nebivolol
MFCD00865796
(S,R,R,R)-NEBIVOLOL-D2,15N HYDROCHLORIDE
Nibivolol
rac-nebivolol
NEBIVOLOLHCL
NEBIVOLOL HYDROCHLORIDE
NEBIVOLOL-D4

Biological Activity

[Description]:

(Rac)-Nebivolol ((Rac)-R 065824) is a racemic isomer of Nebivolol. Nebivolol is a selective β1-adrenergic receptor antagonist with an IC50 value of 0.8 nM. Nebivolol can prevent up-regulation of Nox2/NADPH oxidase and lipoperoxidation in the early stages of ethanol-induced cardiac toxicity. Vasodilatory activity[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

IC50: 0.8 nM (β1-adrenergic receptor)[1]

[In Vivo]

Nebivolol (10 mg/kg; daily for 7 days) markedly improves endothelial dysfunction and increases P-VASP levels; prevents NOS III uncoupling; significantly inhibit NADPH oxidase in Angiotensin II-treated rats[3].

[References]

[1]. do Vale GT, et al. Nebivolol Prevents Up-Regulation of Nox2/NADPH Oxidase and Lipoperoxidation in the Early Stages of Ethanol-Induced Cardiac Toxicity. Cardiovasc Toxicol. 2021 Mar;21(3):224-235.

[2]. Cockcroft JR, et al. Nebivolol vasodilates human forearm vasculature: evidence for an L-arginine/NO-dependent mechanism. J Pharmacol Exp Ther. 1995 Sep;274(3):1067-71.

[3]. Oelze M, et al. Nebivolol inhibits superoxide formation by NADPH oxidase and endothelial dysfunction in angiotensin II-treated rats. Hypertension. 2006 Oct;48(4):677-84.

Chemical & Physical Properties

[ Density]:
1.309 g/cm3

[ Boiling Point ]:
600.5ºC at 760 mmHg

[ Melting Point ]:
155-156°C(lit.)

[ Molecular Formula ]:
C₂₂H₂₅F₂NO₄

[ Molecular Weight ]:
405.43500

[ Flash Point ]:
316.9ºC

[ Exact Mass ]:
405.17500

[ PSA ]:
70.95000

[ LogP ]:
2.75450

[ Index of Refraction ]:
1.58

[ Storage condition ]:
20°C

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.