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Relationship of N ‐demethylation of amiflamine and its metabolite to debrisoquine hydroxylation polymorphism
Author(s) -
Alván G,
Grind M,
Graffner C,
Sjöqvist F
Publication year - 1984
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1984.212
Subject(s) - debrisoquine , hydroxylation , metabolite , demethylation , chemistry , metabolism , pharmacology , urine , biochemistry , biology , cyp2d6 , cytochrome p450 , gene , enzyme , dna methylation , gene expression
The metabolism of the new reversible A‐selective monoamine oxidase inhibitor amiflamine was studied in relation to polymorphic hydroxylation of debrisoquine in 24 healthy subjects. Amiflamine is metabolized by two consecutive N ‐demethylations. By construction of urinary recovery ratios analogous to that of debrisoquine/4‐hydroxydebrisoquine, correlations between debrisoquine metabolic ratio and amiflamine/demethylated metabolites were significant and consistent within slow and rapid hydroxylators of debrisoquine. It is concluded that debrisoquine hydroxylation and amiflamine N ‐demethylation might be under common genetic regulation. Clinical Pharmacology and Therapeutics (1984) 36, 515–519; doi: 10.1038/clpt.1984.212