Carvedilol

Carvedilol (BM14190) is an antagonist of α1- and β-adrenergic receptors (AR) and is used to treat congestive heart failure (CHF) and hypertension [1].

Adrenergic receptors are a class of G protein-coupled receptors, targets of norepinephrine and epinephrine, and are involved in the sympathetic nervous system [2].

In vitro: Carvedilol rapidly inhibited Fe2+-initiated lipid peroxidation in rat brain homogenates, with an IC50 of 8.1 μM. In rat brain homogenates, Carvedilol protected the homogenate from Fe2+-induced α-tocopherol depletion, with an IC50 of 17.6 μM. Carvedilol reduced the intensity of the DMPO-OH signal in a dose-dependent manner, with an IC50 of 25 μM [1]. Carvedilol prevents vascular smooth muscle cell proliferation, migration, and neointimal formation after vascular injury. In cultured human pulmonary artery vascular smooth muscle cells, Carvedilol (0.1-10 μM) inhibited mitogenesis stimulated by platelet-derived growth factor, epidermal growth factor, thrombin, and serum in a concentration-dependent manner, with IC50 values of 0.3-2.0 μM. Carvedilol inhibited platelet-derived growth factor-induced vascular smooth muscle cell migration in a concentration-dependent manner, with an IC50 of 3 μM [3].

References:
[1].? Yue T L, Cheng H Y, Lysko P G, et al. Carvedilol, a new vasodilator and beta adrenoceptor antagonist, is an antioxidant and free radical scavenger[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 263(1): 92-98.
[2].?Furchgott R F. The receptors for epinephrine and norepinephrine (adrenergic receptors)[J]. Pharmacological reviews, 1959, 11(2): 429-441.
[3].?Ohlstein E H, Douglas S A, Sung C P, et al. Carvedilol, a cardiovascular drug, prevents vascular smooth muscle cell proliferation, migration, and neointimal formation following vascular injury[J]. Proceedings of the National Academy of Sciences, 1993, 90(13): 6189-6193.