Article

Fluoroalkylation of Dextromethorphan Improves CNS Exposure and Metabolic Stability

2021-04-28

Abstract excerpt

Aryl-methyl ethers, while present in many bioactive compounds, are subject to rapid O-dealkylation that can generate bio-inactive or toxic metabolites. As an example, the cough suppressant dextromethorphan undergoes such a P450 mediated O-dealkylation to provide the psychoactive phenolic metabolite dextrorphan. This metabolite antagonizes the NMDA receptor causing hallucinations, which encourages recreational abus...

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Literature Corpus work: b19bbbd6-dbfc-5626-a758-8d38ac63f1e8
DOI: 10.26434/chemrxiv.14495748.v1

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