Title : Effects of antidepressant drugs on the activity of cytochrome P-450 measured by caffeine oxidation in rat liver microsomes.

Pub. Date : 2001 Jul-Aug

PMID : 11990081






3 Functional Relationships(s)
Download
Sentence
Compound Name
Protein Name
Organism
1 In the case of 1-N- and in particular 7-N-demethylation of caffeine, apart from CYP1A2, other cytochrome P-450 isoenzymes play a considerable role. Caffeine cytochrome P450, family 1, subfamily a, polypeptide 2 Rattus norvegicus
2 The influence of amitriptyline on 8-hydroxylation and especially on 7-N-demethylation of caffeine was weaker (Ki = 108 and 190 pM, respectively) than on 3-N- or 1-N-demethylation, suggesting a narrower spectrum of cytochrome P-450 inhibition by amitriptyline than by imipramine, involving mainly the subfamily CYP1A2, and--to a lesser degree--CYP3A. Caffeine cytochrome P450, family 1, subfamily a, polypeptide 2 Rattus norvegicus
3 However, fluoxetine displayed a clear inhibitory effect on caffeine 7-N-demethylation (Ki = 72 microM), the reaction which is catalyzed mainly by other than CYP1A2 isoenzymes. Caffeine cytochrome P450, family 1, subfamily a, polypeptide 2 Rattus norvegicus