(S)-(-)-Carvedilol

(S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX)[1].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

β/α-1 adrenergic receptor[1]

The β-receptor blocking activity of (S)-Carvedilol is about 100 times greater than that of (R)-Carvedilol, whereas both enantiomers show equipotent potency as α-blockers[1]. (S)-Carvedilol significantly attenuates Doxorubicin (DOX)-induced cell death, apoptotic morphological changes, decrease the mitochondrial membrane potential and oxidative stress responses by increasing the superoxide dismutase and catalase activities, and decreasing malondialdehyde contents and reactive oxygen species levels via the PI3K/AKT/eNO synthase pathway in vitro[1]. (S)-Carvedilol treatment significantly upregulates the expression levels of p-eNOS in HUVECs[1].

[1]. Wu T, et al. Protective effects of S-carvedilol on doxorubicin-induced damages to human umbilical vein endothelial cells and rats. J Appl Toxicol. 2019 Aug;39(8):1233-1244.