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Structure reactivity relationships in the microsomal oxidation of tertiary amines

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Summary

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.

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Correspondence to Mario Salmona.

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Galliani, G., Rindone, B., Dagnino, G. et al. Structure reactivity relationships in the microsomal oxidation of tertiary amines. European Journal of Drug Metabolism and Pharmacokinetics 9, 289–293 (1984). https://doi.org/10.1007/BF03189678

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Key words

  • Structure-reactivity relationships
  • microsomes
  • dealkylation