ZAHRADNÍKOVÁ, Lucia, Ondřej ZENDULKA, Jan JUŘICA and Eva MCCASKEY HADAŠOVÁ. Gender-dependent influence of bupropion on the activity of hepatic cytochrome P450 2D2 in rats. Activitas Nervosa Superior. 2008, vol. 50, 1-2, p. 23-25. ISSN 1802-9698.
Other formats:   BibTeX LaTeX RIS
Basic information
Original name Gender-dependent influence of bupropion on the activity of hepatic cytochrome P450 2D2 in rats
Name in Czech Vliv bupropionu na aktivitu jaterního cytochromu P450 2D2 u potkana v závislosti na pohlaví
Authors ZAHRADNÍKOVÁ, Lucia (703 Slovakia, guarantor), Ondřej ZENDULKA (203 Czech Republic), Jan JUŘICA (203 Czech Republic) and Eva MCCASKEY HADAŠOVÁ (203 Czech Republic).
Edition Activitas Nervosa Superior, 2008, 1802-9698.
Other information
Original language English
Type of outcome Article in a journal
Field of Study 30104 Pharmacology and pharmacy
Country of publisher Czech Republic
Confidentiality degree is not subject to a state or trade secret
RIV identification code RIV/00216224:14110/08:00027335
Organization unit Faculty of Medicine
Keywords in English cytochrome P450; bupropion
Tags bupropion, cytochrome P450
Changed by Changed by: doc. PharmDr. Ondřej Zendulka, Ph.D., učo 167123. Changed: 12/1/2009 14:51.
Abstract
One of the most important enzymatic systems participating in drug metabolism is cytochrome P450 (CYP450). CYP450 consists of many isoforms which activity of is influenced by numerous endogenous (e.g. gender, pathophysiological status, age) and exogenous factors (e.g. xenobiotical inhibitors and inducers). Although bupropion is not metabolized by CYP 2D6 (human ortologue of rat CYP2D2), there is certain potential for interaction when bupropion is co-administered with other drugs metabolized by this isoenzyme, too. The aim of the present study was to determine the influence of gender and administration of bupropion on the CYP450 isoform 2D2 (CYP2D2) activity. As selective markers of the metabolic activity of CYP2D2 dextromethorphan (DEM) and its metabolite dextrorphane (DOR) were used. In animals treated with bupropion compared to control animals administered with saline the inhibitory effect of bupropion was expressed as a decrease of DOR in the 30th, 60th and 120th minutes of perfusion.
Abstract (in Czech)
Cytochróm P-450 (CYP450) hraje kľúčovú úlohu v biotransformačných procesoch veľkého množstva xenobiotík. Interindividuálna variabilita aktivity oxidatívnych a konjugačných enzýmov, hlavne CYP-450, môže byť zapríčinená rôznymi faktormi ako napr. druh, pohlavie, vek, genetický základ jedinca, alebo interakcie medzi súčastne podávanými liečivami, dosledkom čoho može byť rôzna farmakoterapeutická účinnosť liečiva. Predkladanou prácou by sme radi prispeli k odhaleniu možných zmien metabolickej aktivity enzymatického systému CYP450 konkrétne izoformy 2D2 u potkanov kmeňa Wistar spôsobených vplyvom pohlavia a bupropionu. Ovplyvnenie ľudskej izoformy CYP2D6 bupropionom, má inhibičný efekt. Nami získané výsledky ukazujú, že u kontrolnej skupiny bola koncentrácia metabolitu DOR signifikantne vyššia len v 30 minúte. U samíc sme dokonca zaznamenali vyššiu koncentráciu DOR než u samcov a to v 30 minúte o 32% a v 60 a 120 minúte o 17%.
Links
MSM0021622404, plan (intention)Name: Vnitřní organizace a neurobiologické mechanismy funkčních systémů CNS
Investor: Ministry of Education, Youth and Sports of the CR, The internal organisation and neurobiological mechanisms of functional CNS systems under normal and pathological conditions.
PrintDisplayed: 25/7/2024 22:14