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Nebivolol hydrochloride

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Nebivolol hydrochloride Basic information

Product Name:
Nebivolol hydrochloride
Synonyms:
  • Narbivolol
  • rel-(aR,a′R,2R,2′S)-a,a′-[iminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] hydrochloride
  • Nebivolol hydrochloride, >=98%
  • RAC NEBIVOLOL, HYDROCHLORIDE
  • a,a(Iminodimethylene)bis[6-fluoro-2-chromanmethanol] Hydrochloride
  • Lobivon
  • Nebilet
  • Nebilox
CAS:
152520-56-4
MF:
C22H26ClF2NO4
MW:
441.9
EINECS:
1806241-263-5
Product Categories:
  • R-67145
  • API
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • 152520-56-4
Mol File:
152520-56-4.mol
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Nebivolol hydrochloride Chemical Properties

Melting point:
220-222°C
storage temp. 
room temp
solubility 
DMSO: ≥20mg/mL
form 
powder
color 
white to off-white
Merck 
14,6432
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Safety Information

Hazard Codes 
Xn,N
Risk Statements 
22-50/53
Safety Statements 
60-61
RIDADR 
3077
WGK Germany 
3
HS Code 
29322090
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Nebivolol hydrochloride Usage And Synthesis

Chemical Properties

White to Off-White Powder

Uses

A ?-Adrenergic blocker. Used as an antihypertensive

Uses

Nebivolol Hydrochloride is a highly selective β1-adrenoceptor antagonist.

Uses

Nebivolol selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM

Definition

ChEBI: (R,S,S,S)-nebivolol hydrochloride is a hydrochloride obtained by reaction of (R,S,S,S)-nebivolol with one equivalent of hydrochloric acid. It contains a (R,S,S,S)-nebivolol(1+). It is an enantiomer of a (S,R,R,R)-nebivolol hydrochloride.

Biological Activity

Highly selective β 1 -adrenoceptor antagonist (K i values are 0.88, 20, 44, 700, 1160, 2400 and 4000 nM at β 1 , 5-HT 1A , β 2 , 5-HT 2 , α 1 , H 1 and D 2 receptors respectively). Induces vasodilation via a nitric oxide- and cGMP-dependent mechanism (EC 50 = 11.36 μ M in renal arteries) and displays antihypertensive activity in vivo .

Biochem/physiol Actions

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.

storage

Desiccate at RT

Nebivolol hydrochlorideSupplier

Shanghaizehan biopharma technology co., Ltd. Gold
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