Chemical Properties
White to Off-White Powder
Uses
A ?-Adrenergic blocker. Used as an antihypertensive
Uses
Nebivolol selectively inhibits β1-adrenoceptor with IC50 of 0.8 nM
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 .
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.
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.
