Biological activity | (S)-Carvedilol is a Carvedilol S-type isomer, a non-selective β/α-1 receptor blocker. (S)-Carvedilol can resist vascular or cardiac toxicity of Doxorubicin (DOX). |
target | β/α-1 adrenergic receptor |
in vitro study | The β-receptor blocking activity of (S)-Carvedilol is about 100 times greater that of (R)-Carvedilol, whereas both enantiomers show equipotent potency as α-blockers. (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. (S)-Carvedilol treatment significantly upregulates the expression levels of p-eNOS in HUVECs. |
use | the optically active isomer of Carvedilol (C184625), a nonselective β-adrenertic blocker with a1-blocking activity. an antihypertensive used in the treatment of congestive heart failure. |