Carvedilol is a potent nonselective β1-, β2-, and α1- adrenoceptor antagonist drug with an IC50 value of 3.8 µM. Carvedilol is also vasodilator with antioxidant, anti-inflammatory, antifibrotic and antiproliferative effects. It has “atypical” effects on β-receptors mediated by an interaction with G proteins that leads to downregulation of receptors in model systems. Experimental models demonstrate that Carvedilol blocks α1-, β1-, and β2-adrenergic receptors without exhibiting high levels of inverse agonist activity. The lack of inverse agonist activity and intrinsic sympathomimetic activity (ISA) reduces the side-effects and makes the compound better tolerated than the older β-blockers. The pharmacologic effects of carvedilol are related to the inhibition of multiple neurohormonal pathways. Additional studies indicate that some of the efficacy of carvedilol may be associated with its effects on levels of inflammatory cytokines. Carvedilol also blocks KV1. channels independently of its action on adrenoceptors5, as well as Kir2.3 channels.
产品描述
A Blocker of KV1.5 and Kir2.3 Channels and an Antagonist of Adrenoceptors
产品形式
Carvedilol is a potent nonselective β1-, β2-, and α1- adrenoceptor antagonist drug with an IC50 value of 3.8 µM. Carvedilol is also vasodilator with antioxidant, anti-inflammatory, antifibrotic and antiproliferative effects. It has “atypical” effects on β-receptors mediated by an interaction with G proteins that leads to downregulation of receptors in model systems. Experimental models demonstrate that Carvedilol blocks α1-, β1-, and β2-adrenergic receptors without exhibiting high levels of inverse agonist activity. The lack of inverse agonist activity and intrinsic sympathomimetic activity (ISA) reduces the side-effects and makes the compound better tolerated than the older β-blockers. The pharmacologic effects of carvedilol are related to the inhibition of multiple neurohormonal pathways. Additional studies indicate that some of the efficacy of carvedilol may be associated with its effects on levels of inflammatory cytokines. Carvedilol also blocks KV1. channels independently of its action on adrenoceptors5, as well as Kir2.3 channels.