carvedilol

Carvedilol (SKF 105517) Phosphate is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and devoid of intrinsic sympathomimetic activity. The S enantiomer of carvedilol nonselectively binds to and blocks beta-adrenergic receptors, thereby exerting negative inotropic and chronotropic effects, and leading to a reduction in cardiac output. In addition, both enantiomers of carvedilol bind to and block alpha 1-adrenergic receptors, thereby causing vasodilation and reducing peripheral vascular resistance.

(S)-Carvedilol is a non-selective β α-1 blocker.It exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).

Carvedilol EP IMpurity E (Carvedilol USP E) is used as a pharmaceutical intermediate.

(R)-Carvedilol is a non-selective blocker of β α-1. (R)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX).

Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is the phosphate salt form of carvedilol, a racemic mixture and adrenergic blocking agent with antihypertensive activity and no intrinsic sympathomimetic activity.

4-Hydroxyphenyl Carvedilol, a metabolite of Carvedilol, is associated with the pharmacological activity of this beta-blocker alpha-1 blocker.

4-Hydroxyphenyl Carvedilol D5 is the deuterium labeled 4-Hydroxyphenyl Carvedilol.

(R,S)-Carvedilol glucuronide is a racemic mixture of the carvedilol metabolites (R)-carvedilol glucuronide and (S)-carvedilol glucuronide. (R)-Carvedilol glucuronide is formed via glucuronidation of (R)-carvedilol by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT2B4. (S)-Carvedilol glucuronide is formed via glucuronidation of (S)-carvedilol by UGT2B4 and UGT2B7.

O-Desmethylcarvedilol (Desmethylcarvedilol) is an active metabolite of Carvedilol, a non-selective β-adrenergic receptor (β-AR) antagonist. This compound inhibits store overload-induced calcium release in HEK293 cells expressing the RyR2 R4496C mutation (IC50= 7.62 µM). Additionally, O-Desmethylcarvedilol slows the increase in heart rate and prevents diastolic pressure reduction induced by Isoproterenol in conscious rabbits (ED50s = 32 and 5 µg kg).

SB 211475, a metabolite of carvedilol, is a novel antihypertensive agent and a potent antioxidant.

VK-II-36, a carvedilol analog, suppresses sarcoplasmic reticulum (SR) Ca(2+) release but does not block the β-receptor.

Homo-VK-II-36 (Homo-V-II-36) is a carvedilol analogue that acts by inhibiting store- overload-induced calcium release through the RyR2 channel.

VK-II-86 is a non-β-blocking carvedilol analog. It prevents ouabain-Induced cardiotoxicity