Deeper Insight into the Reducing Biotransformation of Bupropion in the Human Liver

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11160%2F14%3A10281977" target="_blank" >RIV/00216208:11160/14:10281977 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.jstage.jst.go.jp/article/dmpk/29/2/29_DMPK-13-RG-051/_html" target="_blank" >http://www.jstage.jst.go.jp/article/dmpk/29/2/29_DMPK-13-RG-051/_html</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.2133/dmpk.DMPK-13-RG-051" target="_blank" >10.2133/dmpk.DMPK-13-RG-051</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Deeper Insight into the Reducing Biotransformation of Bupropion in the Human Liver

Popis výsledku v původním jazyce

Bupropion is widely used as an antidepressant drug and also as a smoking cessation aid. In humans, this drug is extensively metabolized to form several metabolites. Oxidised hydroxybupropion and two reduced metabolites, threohydrobupropion and erythrohydrobupropion, are major metabolites. All of these metabolites are considered to be active. Although the oxidative metabolic pathway and the central role of CYP2B6 are known, the enzymes that participate in the reduction have not been identified to date. The aim of this study was to confirm the role of human liver subcellular fractions in the metabolism of bupropion and elucidate the contribution of particular carbonyl-reducing enzymes. An HPLC method for the determination of bupropion metabolites was utilised. Bupropion is reduced to threohydrobupropion and less to erythrohydrobupropion in human liver cytosol, microsomes and also mitochondria. Surprisingly, intrinsic clearance for formation of both metabolites is the highest in mitochond

Název v anglickém jazyce

Deeper Insight into the Reducing Biotransformation of Bupropion in the Human Liver

Popis výsledku anglicky

Bupropion is widely used as an antidepressant drug and also as a smoking cessation aid. In humans, this drug is extensively metabolized to form several metabolites. Oxidised hydroxybupropion and two reduced metabolites, threohydrobupropion and erythrohydrobupropion, are major metabolites. All of these metabolites are considered to be active. Although the oxidative metabolic pathway and the central role of CYP2B6 are known, the enzymes that participate in the reduction have not been identified to date. The aim of this study was to confirm the role of human liver subcellular fractions in the metabolism of bupropion and elucidate the contribution of particular carbonyl-reducing enzymes. An HPLC method for the determination of bupropion metabolites was utilised. Bupropion is reduced to threohydrobupropion and less to erythrohydrobupropion in human liver cytosol, microsomes and also mitochondria. Surprisingly, intrinsic clearance for formation of both metabolites is the highest in mitochond

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

CE - Biochemie

OECD FORD obor

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Projekt

<a href="/cs/project/EE2.3.20.0235" target="_blank" >EE2.3.20.0235: Vybudování výzkumného týmu experimentální a aplikované biofarmacie</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2014

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Drug metabolism and pharmacokinetics

ISSN

1347-4367

e-ISSN

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Svazek periodika

29

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

JP - Japonsko

Počet stran výsledku

8

Strana od-do

177-184

Kód UT WoS článku

000334596600011

EID výsledku v databázi Scopus

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