Cell lines

human neutrophils

Preparation method

The solubility of this compound in DMSO is >20.3mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

10~100μM

Applications

Carvedilol inhibited PMA-induced O2- production in human neutrophils in a dose-dependent manner with an IC50 value of 28μM.

Animal models

Lewis rats induced with acute experimental autoimmune myocarditis

Dosage form

20 mg/kg/day for 3 wk

Application

Carvedilol suppressed left ventricular fractional shortening and decreased heart rates, markedly reduced the severity of myocarditis and suppressed thickening of the left ventricular posterior wall in rats with experimental autoimmune myocarditis.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

Carvedilol(BM14190), an antagonist ofα1- and β-adrenergic receptors (ARs), is used to treat congestive heart failure (CHF) and high blood pressure [1].

Adrenergic receptors, a class of G protein-coupled receptors, are targets of thenorepinephrine and epinephrine which have been involved in sympathetic nervous system[2]..

In vitro: Carvedilol potently inhibited Fe2+-initiated lipid peroxidation in rat brain homogenate with an IC50 of 8.1 μM. In rat brain homogenate, carvedilol protected against Fe2+-induced α-tocopherol depletion with an IC50 of 17.6 μM. Carvedilol dose-dependently decreased the intensity of the DMPO-OH signal, with an IC50 of 25 μM [1]. Carvedilol prevented vascular smooth muscle cell migration, proliferation, and neointimal formation following vascular injury. In human cultured pulmonary artery vascular smooth muscle cells, carvedilol (0.1-10 μM) concentration-dependently inhibited the mitogenesis stimulated by platelet-derived growth factor, epidermal growth factor, thrombin, and serum, with IC50 values ranging from 0.3 to 2.0 μM. Carvedilol concentration-dependently inhibited vascular smooth muscle cell migration induced by platelet-derived growth factor with an IC50 value 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