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Carvedilol (phosphate hemihydrate) (BM 14190 (phosphate hemihydrate)) is a non-selective beta blocker/alpha-1 blocker with an IC50 of 3.8 μM for inhibition of LDL oxidation. IC50: 3.8 μM (beta Adrenergic Receptor).

Carvedilol (BM 14190) is a nonselective-blocking agent and is used in the treatment of hypertension and angina pectoris. As a third-generation β-adrenergic blocker (β-blocker), Carvedilol is able to reverse cardiac structural remodeling. Recentresults demonstrated that the effect caused by Carvedilol on cardiac remodeling is largely dependent on endogenous NO.

[1]. Chen J, et al. The effects of carvedilol on cardiac structural remodeling: The role of endogenous nitric oxide in the activity of carvedilol. Mol Med Rep. 2013 Apr;7(4):1155-1158. [2]. Stafylas PC, et al. Carvedilol in hypertension treatment. Vasc Health Risk Manag. 2008;4(1):23-30. [3]. Othman AA, et al. Population pharmacokinetics of S(-)-carvedilol in healthy volunteers after administration of the immediate-release (IR) and the new controlled-release (CR) dosage forms of the racemate. AAPS J. 2007 Jun 15;9(2):E208-18. [4]. Koshimizu TA, et al. Carvedilol selectively inhibits oscillatory intracellular calcium changes evoked by human alpha1D- and alpha1B-adrenergic receptors. Cardiovasc Res. 2004 Sep 1;63(4):662-672.

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