(rac)-Nebivolol-d8

Names

[ CAS No. ]:
1219166-00-3

[ Name ]:
(rac)-Nebivolol-d8

[Synonym ]:
2-[[2-hydroxy-2-(3,3,4,4-tetradeuterio-6-fluoro-2H-chromen-2-yl)ethyl]amino]-1-(3,3,4,4-tetradeuterio-6-fluoro-2H-chromen-2-yl)ethanol

Biological Activity

[Description]:

(Rac)-Nebivolol-d8 ((rac)-R 065824-d8) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Research Areas >> Endocrinology
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[In Vitro]

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

[References]

[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Brehm BR, et al. Effects of nebivolol on proliferation and apoptosis of human coronary artery smooth muscle and endothelial cells. Cardiovasc Res. 2001 Feb 1;49(2):430-9.

[3]. Mercanoglu G, et al. The effects of nebivolol on apoptosis in a rat infarct model. Circ J. 2008 Apr;72(4):660-70.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H17D8F2NO4

[ Molecular Weight ]:
413.48400

[ Exact Mass ]:
413.22500

[ PSA ]:
70.95000

[ LogP ]:
2.75450

Related Compounds