(Rac)-Nebivolol-d4 ((Rac)-R 065824-d4) 是 Nebivolol 氘代消旋体。Nebivolol 是 β1-肾上腺素受体选择性抑制剂，IC50 为 0.8 nM。
(Rac)-Nebivolol-d4 ((Rac)-R 065824-d4) is a labelled racemic Nebivolol. Nebivolol selectively inhibits β1- adrenergic receptor with IC50 of 0.8 nM[1][2].
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].
[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.
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