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Merck
CN

N1915

Sigma-Aldrich

Nebivolol hydrochloride

≥98% (HPLC)

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别名:
Narbivolol, Nebilet, R-65824, rel-(aR,a′R,2R,2′S)-a,a′-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] hydrochloride
经验公式(希尔记法):
C22H25F2NO4 · HCl
分子量:
441.90
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to off-white

溶解性

DMSO: ≥20 mg/mL

创始人

Forest Labs

储存温度

room temp

SMILES字符串

Cl.O[C@@H](CNC[C@H](O)[C@@H]1CCc2cc(F)ccc2O1)[C@H]3CCc4cc(F)ccc4O3

InChI

1S/C22H25F2NO4.ClH/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22;/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2;1H/t17-,18-,21-,22+;/m0./s1

InChI key

JWEXHQAEWHKGCW-BIISKSHESA-N

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应用

Nebivolol hydrochloride has been used as a standard in the validation of high-performance thin-layer chromatography (HPTLC)-densitometry method. It may be used in calibration curve preparation and absorption spectrum studies using spectrophotometry.

生化/生理作用

Nebivolol hydrochloride (NEB) is used as a racemic mixture for clinical studies. It stabilizes membrane and possesses intrinsic sympathomimetic functionality. Nebivolol interaction with π-acceptors (2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), 2,4-dinitrophenol (DNP) and 2,4,6-trinitrophenol (picric acid; PA)) is useful in the spectrophotometric detection methods.
Nebivolol is a competitive, highly selective b1-receptor antagonist with mild vasodialating properties, possibly due to an interaction with the L-arginine/ NO pathway, and is used for treatment of essential hypertension. It is 40-fold selective for β1 vs. β2, and lacks ISA (intrinsic sympathomimetic activity).

特点和优势

This compound is featured on the β-Adrenoceptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Forest Labs. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

WGK

WGK 3

法规信息

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Development of quantitative HPTLC-Densitometry methods for the analysis of amiodarone HCl, carvedilol, doxylamine succinate, magnesium salicylate, metoprolol succinate, nebivolol HCl, and salicylamide using a model process developed earlier for the transfer of TLC screening methods
Nguyen K and Sherma J
Acta Chromatographica , 30(4), 264-268 (2018)
Nebivolol Hydrochloride Loaded Nanostructured Lipid Carriers as Transdermal Delivery System: Part 1: Preparation, Characterization and In Vitro Evaluation
Ghazy E, et al.
Al-Mustansiriyah Journal of Pharmaceutical Sciences (AJPS), 16(2), 14-Jan-14-Jan (2016)
New spectrophotometric determination of nebivolol in pharmaceutical formulation via charge transfer complex
Alhemiary, Nabil AF
Austin Journal of Analytical and Pharmaceutical Chemistry , 4(2), 1084-1091 (2017)
Vijay Singh Jatav et al.
Advanced biomedical research, 2, 62-62 (2013-11-14)
Nebivolol hydrochloride is a third generation β-blocker with highly selective β1-receptor antagonist with antihypertensive properties having plasma half life of 10 h and 12% oral bioavailability. The aim of the present investigation was to form matrix type transdermal patches containing
Jillian G Baker et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 25(12), 4486-4497 (2011-08-26)
β-Adrenoceptor antagonists differ in their degree of partial agonism. In vitro assays have provided information on ligand affinity, selectivity, and intrinsic efficacy. However, the extent to which these properties are manifest in vivo is less clear. Conscious freely moving rats

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