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Usage

Uses

Used in Pharmaceutical Industry:
(R)-(+)-4'-HYDROXYPHENYL-CARVEDILOL is used as an active pharmaceutical ingredient for the treatment of hypertension. As a metabolite of Carvedilol, it possesses a more potent β-adrenergic receptor antagonist effect, making it a valuable compound in managing high blood pressure.
Used in Cardiovascular Applications:
(R)-(+)-4'-HYDROXYPHENYL-CARVEDILOL is used as a therapeutic agent for cardiovascular conditions due to its β-adrenergic receptor antagonist properties. It helps in the treatment of hypertension by blocking the effects of adrenaline on the heart, leading to a decrease in heart rate and blood pressure.
Used in Research and Development:
(R)-(+)-4'-HYDROXYPHENYL-CARVEDILOL is used as a research compound for studying the effects of β-adrenergic receptor antagonists on various physiological processes. Its ability to inhibit the formation of DPPH radicals makes it a useful tool in understanding the antioxidant properties of related compounds and their potential applications in medicine.

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Relevant academic research and scientific papers

Suppression of store overload-induced calcium release by hydroxylated metabolites of carvedilol

Carvedilol is a drug widely used in the treatment of heart failure and associated cardiac arrhythmias. A unique action of carvedilol is its suppression of store overload-induced calcium release (SOICR) through the cardiac ryanodine receptor (RyR2), which can trigger ventricular arrhythmias. Since the effects of carvedilol metabolites on SOICR have not yet been investigated, three carvedilol metabolites hydroxylated at the 3-, 4′ and 5′-positions were synthesized and assayed for SOICR inhibition in mutant HEK 293 cells expressing the RyR2 mutant R4496C. This cell line is especially prone to SOICR and calcium release through the defective RyR2 channel was measured with a calcium-sensitive fluorescent dye. These results revealed that the 3- and 4′-hydroxy derivatives are slightly more effective than carvedilol in suppressing SOICR, while the 5′-analog proved slightly less active. Metabolic deactivation of carvedilol via these hydroxylation pathways is therefore insignificant.

Synthesis of active metabolites of carvedilol, an antihypertensive drug

A simple synthetic route for active metabolites of carvedilol is reported. The metabolites 4'-hydroxycarvedilol and 5'-hydroxycarvedilol have exhibited high activity for -blockade. We have disclosed syntheses of 4'-hydroxycarvedilol and 5'-hydroxycarvedil