Небиволол

Nebilet was launched in Germany and the Netherlands as an antihypertensive agent. It is prepared by a five step route starting with 6-fluoro-4- oxobenzopyran-2-carboxylic acid. It is a selective β₁-adrenergic receptor antagonist and is 50 times less potent at β₂-receptors. Vasodialating properties occur via the nitric oxide pathway. While the L-isomer is more potent than the D-isomer, the racemic mixture is necessary for optimal activity. Upon administration, an immediate fall in blood pressure occurs, it improves both left ventricular systolic and diastolic function, and lowers peripheral blood resistance. Nebilet does not influence insulin sensitivity nor lipid profile comparible to atenolol. Doses of 50 mg of atenolol and 10 mg of Nebilet are equipotent but Nebilet has a longer duration of action due to an accumulation of the drug and increasing plasma levels of active metabolites.

Labeled Nebivolol, intended for use as an internal standard for the quantification of Nebivolol by GC- or LC-mass spectrometry.

ChEBI: A member of the class of chromanes that is 2,2'-iminodiethanol in which one hydrogen attached to each hydroxy-bearing carbon is replaced by a 6-fluorochroman-2-yl group.