Influence of 5-HT1 receptor agonists on the activity of CYP2D1 and N-acetyltransferase in the isolated perfused rat liver

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14110%2F01%3A00005509" target="_blank" >RIV/00216224:14110/01:00005509 - isvavai.cz</a>
Result on the web
—
DOI - Digital Object Identifier
—

Result language
angličtina
Original language name
Influence of 5-HT1 receptor agonists on the activity of CYP2D1 and N-acetyltransferase in the isolated perfused rat liver
Original language description
The study was aimed to determine if the pretreatment with the selected 5-HT1 receptor agonists, CGS 12066B (5-HT1B), RU-24969 (5-HT1A/B and sumatriptan (5-HT1B/D), may affect oxidative and/or conjugative drug metabolism in the isolated perfused rat liver. Cytochrome P450 2D1-mediated O-demethylation of dextromethorphan (DEM)to dextrorphan (DOR), and arylamine N-acetyltransferase (NAT2)-mediated N-acetylation of procainamide (PA) to N-acetylprocainamide (NAPA), were used as representative, clinically important, metabolic reactions. The results showed a significant decrease in O-demethylation of DEM to DOR in all measured intervals (30 - 60 - 120 min) of the liver perfusion after the pretreatment with selective 5-HT1B agonist CGS 12066B and 5-HT1A/B agonist RU-24969. Sumatriptan however had no substantial effect on the CYP2D1 O-demethylation activity. The effect of 5-HT1 agonists on the N-acetylation of procainamide (substrate for NAT2), was much less marked; CGS 12066B and sumatriptan p
Czech name
—
Czech description
—

Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FR - Pharmacology and apothecary chemistry
OECD FORD branch
—

Publication year
2001
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Similar results(10)