Vergleichende Demethylierung von tricyclischen Psychopharmaka durch Rattenleber-Mikrosomen
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Zusammenfassung
Zwölf tricyclische Psychopharmaka mit tertiärer Aminfunktion und ihre Desmethylderivate (sekundäre Amine) wurden auf ihre Demethylierung durch Rattenleber-Mikrosomen (9000 × g-Überstand) untersucht. Alle getesteten tertiären Amin-Derivate werden stark demethyliert, während dies bei ihren Desmethylderivaten (sekundäre Amine) in viel geringerem Ausmaß der Fall ist. Mögliche Auswirkungen auf die pharmakologischen und klinischen Wirkungen dieser Pharmaka werden diskutiert.
Summary
The demethylation of twelve tricyclic psychotropic drugs and their desmethyl derivatives has been investigated using rat liver microsomes (9000 × g Supernatant). All the tested products (tertiary amines) undergo considerable demethylation, whereas this process is much less pronounced in the case of their desmethyl derivatives (secondary amines). Possible relationships with the pharmacological and clinical effects of these drugs are discussed.
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