Carvedilol is a AR (α1 and β-adrenergic receptor) antagonist with antioxidant properties. Studies show that the receptors α1D-AR and α1B-AR have a greater affinity for Carvedilol in comparison to the receptor β1-AR subtype. Carvedilol has been observed to block the oscillatory intracellular calcium changes induced by α1D-AR and α1B-AR, and shown to have a higher oxidative effect than Atenolol (sc-204895). The S(-) enantiomer of Carvedilol acts as a β-blocker, and the R(+) and S (-) enantionmers both block the α1. Carvedilol is an inhibitor of α1B-AR, β1-AR, β2-AR and α1D-AR.
1. Koshimizu, T.A., et al. 2004. Cardiovasc. Res. 63: 662-672. PMID: 15306222 2. Shannon, R. and Chaudhry, M. 2006. Am. Heart J. 152: 842-850. PMID: 17070143 3. Jonsson, G., et al. 2007. J. Cardiovasc. Pharmacol. 49: 27-32. PMID: 17261960 4. Othman, A.A., et al. 2007. AAPS J. 9: E208-E218. PMID: 17614362 5. Stafylas, P.C., et al. 2008. Vasc Health Risk Manag. 4: 23-30. PMID: 18629377
Soluble in DMSO (>25 mg/ml), ethanol (10 mg/ml), methanol (33.8 mg/ml), phosphate buffer (pH 4) (0.43 mg/ml) at 37° C, water (partly miscible), chloroform, methylene chloride, and ethyl ether (slightly soluble). Insoluble in isopropanol.
Store at room temperature
1.25 g/cm3 (Predicted)
n20D 1.66 (Predicted)
Sodium channel protein type VIII alpha subunit: IC50 = 306 nM (rat); HERG: IC50 = 350 nM (human)
Rated 5 out of
DingDing, Q. et al. (PubMed 26327764) reported that the 1- and -adrenergic receptor antagonist Carvedilol may attenuate liver cirrhosis by inhibiting angiogenesis through the VEGF-Src-ERK signaling pathway. -SCBT Publication Review
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