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

Result code in 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>

Result on the web

<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>

Result language

angličtina

Original language name

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

Original language description

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

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

CE - Biochemistry

OECD FORD branch

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Project

<a href="/en/project/EE2.3.20.0235" target="_blank" >EE2.3.20.0235: Establishment of Research Team Focused on Experimental and Applied Biopharmacy</a><br>

Continuities

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

Publication year

2014

Confidentiality

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

Name of the periodical

Drug metabolism and pharmacokinetics

ISSN

1347-4367

e-ISSN

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Volume of the periodical

29

Issue of the periodical within the volume

2

Country of publishing house

JP - JAPAN

Number of pages

8

Pages from-to

177-184

UT code for WoS article

000334596600011

EID of the result in the Scopus database

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