The Effects of Trimethadione and Its Metabolite on Human Liver Debrisoquine 4-Hydroxylase Activity In Vitro

Shinichi KOBAYASHI; Stephen MURRAY; David WATSON; Dorothea SESARDIC; Alan R. BOOBIS; Donald S. DAVIES; Hajime YASUHARA

doi:10.15369/sujms1989.2.27

The Effects of Trimethadione and Its Metabolite on Human Liver Debrisoquine 4-Hydroxylase Activity In Vitro

Shinichi KOBAYASHI, Stephen MURRAY, David WATSON, Dorothea SESARDIC, Alan R. BOOBIS, Donald S. DAVIES, Hajime YASUHARA

著者情報

キーワード: trimethadione, debrisoquine 4-hydroxylase, human liver

ジャーナルフリー

1990 年 2 巻 1 号 p. 27-30

DOI https://doi.org/10.15369/sujms1989.2.27

詳細

抄録

The effects of trimethadione (TMO) and its metabolite, dimethadione (DMO), on human liver microsomal debrisoquine 4-hydroxylase (cytochrome P-450_db1) activity were studied. Inhibition curves showed that there is no significant decrease in the activity of debrisoquine 4-hydroxylase by TMO or DMO (0.1μM to 10mM) . These data suggest that debrisoquine 4-hydroxylase in human liver is not responsible for N-demethylation of TMO, nor are TMO or DMO bound to its active site.

責任著者(Corresponding author)

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