Structure reactivity relationships in the microsomal oxidation of tertiary amines

Guido Galliani, Bruno Rindone, Gustavo Dagnino, Mario Salmona

Research output: Contribution to journalArticle

Abstract

Apparent kinetic parameters Vmax and KM have been measured for the oxidative N-demethylation of twelve para-substituted N, N-dimethylanilines catalysed by rat liver microsomes. Vmax was enhanced by pretreatment of the rats with phénobarbital, whereas pretreatment with β-naphthoflavone gave no appreciable enhancement. In the case of phénobarbital pretreatment the kinetic parameters could be expressed in terms of lipophilic and electronic effect of the substituents. Kinetic parameters from control and β-naphthoflavone microsomes gave no statistically meaningful correlation.

Original languageEnglish
Pages (from-to)289-293
Number of pages5
JournalEuropean Journal of Drug Metabolism and Pharmacokinetics
Volume9
Issue number4
DOIs
Publication statusPublished - Oct 1984

Keywords

  • dealkylation
  • microsomes
  • Structure-reactivity relationships

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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