Influence of 5-HT1 receptor agonists on the activity of CYP2D1 and N-acetyltransferase in the isolated perfused rat liver
Identifikátory výsledku
Kód výsledku v 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>
Výsledek na webu
—
DOI - Digital Object Identifier
—
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Influence of 5-HT1 receptor agonists on the activity of CYP2D1 and N-acetyltransferase in the isolated perfused rat liver
Popis výsledku v původním jazyce
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
Název v anglickém jazyce
Influence of 5-HT1 receptor agonists on the activity of CYP2D1 and N-acetyltransferase in the isolated perfused rat liver
Popis výsledku anglicky
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
Klasifikace
Druh
J<sub>x</sub> - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)
CEP obor
FR - Farmakologie a lékárnická chemie
OECD FORD obor
—
Návaznosti výsledku
Projekt
—
Návaznosti
Z - Vyzkumny zamer (s odkazem do CEZ)
Ostatní
Rok uplatnění
2001
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
Homeostasis
ISSN
0960-7560
e-ISSN
—
Svazek periodika
2000
Číslo periodika v rámci svazku
6
Stát vydavatele periodika
CZ - Česká republika
Počet stran výsledku
3
Strana od-do
261
Kód UT WoS článku
—
EID výsledku v databázi Scopus
—