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  Teresita Carrillo-Hernández,Philippe Schaeffer,Pierre Albrecht Chem. Commun., 2001, 1976-1977
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• Solvents and Organic Chemicals Organic Compounds Organoheterocyclic compounds Indoles and derivatives Carbazoles

Recent Advances in the Study of O-Desmethyl Carvedilol (CAS: 72956-44-6)

O-Desmethyl Carvedilol (CAS: 72956-44-6), a major active metabolite of the widely used beta-blocker carvedilol, has garnered increasing attention in recent years due to its unique pharmacological properties and potential therapeutic applications. This research brief aims to synthesize the latest findings on this compound, focusing on its pharmacokinetics, pharmacodynamics, and clinical implications.

Recent studies have elucidated the metabolic pathways of carvedilol, highlighting the significance of O-Desmethyl Carvedilol as a key intermediary. The compound is formed primarily through CYP2D6-mediated O-demethylation of carvedilol, and its plasma concentrations have been shown to correlate with the therapeutic effects observed in patients. Advanced analytical techniques, including LC-MS/MS, have enabled more precise quantification of this metabolite in biological matrices, facilitating better understanding of its role in carvedilol's overall efficacy.

Pharmacodynamic investigations reveal that O-Desmethyl Carvedilol retains significant β-adrenergic receptor blocking activity while demonstrating altered α1-adrenergic receptor affinity compared to its parent compound. This unique receptor profile may contribute to the differential therapeutic effects observed in various patient populations. Recent in vitro studies suggest that the metabolite may possess enhanced antioxidant properties, potentially offering additional cardiovascular protection beyond its hemodynamic effects.

Clinical research has focused on the interindividual variability in O-Desmethyl Carvedilol formation, particularly in relation to CYP2D6 polymorphisms. Population pharmacokinetic studies have identified significant differences in metabolite exposure among CYP2D6 poor metabolizers, intermediate metabolizers, and ultra-rapid metabolizers. These findings have important implications for personalized dosing strategies, especially in diverse patient populations receiving carvedilol therapy.

The therapeutic potential of O-Desmethyl Carvedilol as a standalone agent is currently under investigation. Preclinical studies in animal models of heart failure have demonstrated promising results, with the metabolite showing comparable or superior efficacy to carvedilol in certain parameters. These findings have spurred interest in developing O-Desmethyl Carvedilol as a novel therapeutic agent, potentially offering advantages in terms of reduced metabolic variability and more predictable pharmacokinetics.

Analytical chemistry advancements have enabled more comprehensive characterization of O-Desmethyl Carvedilol's physicochemical properties. Recent studies have determined its solubility profile across various pH conditions, stability characteristics, and crystal structure. These investigations are crucial for formulation development and quality control in potential future pharmaceutical applications.

Emerging research suggests potential applications of O-Desmethyl Carvedilol beyond cardiovascular medicine. Preliminary studies indicate possible neuroprotective effects in models of neurodegenerative diseases, possibly related to its antioxidant properties and ability to modulate cerebral blood flow. While these findings are promising, further research is needed to fully elucidate these potential therapeutic applications.

In conclusion, O-Desmethyl Carvedilol represents a pharmacologically active metabolite with distinct properties that may contribute significantly to the therapeutic effects of carvedilol. The growing body of research underscores the importance of considering metabolite profiles in drug development and clinical practice. Future studies should focus on further characterizing its pharmacological actions, exploring its standalone therapeutic potential, and investigating its role in personalized medicine approaches to carvedilol therapy.

• 123372-14-5((R)-(+)-O-Desmethyl Carvedilol)
• 918903-20-5(Carvedilol Bis-carbazole)
• 1261395-96-3(4-Hydroxycarvedilol D5)
• 142227-51-8(5’-Hydroxyphenyl Carvedilol)
• 142227-49-4(4’-Hydroxyphenyl Carvedilol)
• 146574-43-8(3-Hydroxy Carvedilol)
• 929106-58-1(Carvedilol-d5)
• 123372-13-4((S)-(-)-O-Desmethyl Carvedilol)
• 95094-00-1((S)-Carvedilol)
• 95093-99-5((R)-Carvedilol)