INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15110%2F07%3A00004264" target="_blank" >RIV/61989592:15110/07:00004264 - isvavai.cz</a>

Result on the web

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DOI - Digital Object Identifier

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Result language

angličtina

Original language name

INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG

Original language description

Nabumetone (4-(6-methoxy-2- naphtyl)-butan-2-one) is a nonsteroidal anti-infl ammatory prodrug, clinically used mainly for treatment of osteoarthritis or rheumatoid arthritis to reduce pain and infl ammation. It undergoes rapid and extensive fi rst-passmetabolism in liver to form the main circulating active metabolite 6-methoxy-2-naphthylacetic acid (6-MNA), which is a potent inhibitor of cyclooxygenase (COX-2). Three main metabolic pathways of nabumetone were described: O-demethylation, reduction of ketone to an alcohol, and an oxidative cleavage of the side-chain1. Possible interactions of nabumetone with liver microsomal cytochromes P450 (CYPs, which are often responsible not only for drug metabolism, but also for unwanted eff ects such an enzyme inhibition or induction2) are studied here at the level of human and pig liver microsomes. To prove the suitability of pig as an experimental model for following of metabolism and pharmacokinetics of drugs we compared the inhibition of a

Czech name

Interakce nabumetonu s cytochromy P450 in vitro: srovnání u člověka a prasete

Czech description

Nabumeton je nesteroidní protizánětlivé léčivo používané k léčbě osteoartritidy a revmatoidní artritidy k mírnění zánětu a bolesti. V práci je sledována interakce nabumetonu s jaterními mikrosomálními cytochromy P450 u člověka a prasete. Většina enzymových aktivit CYP450 je ovlivněna stejně jak u člověka tak u prasete , což z prasete činí vhodný model pro studium metabolismu a kinetiky tohoto léčiva.

Type

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

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

<a href="/en/project/1P05OC050" target="_blank" >1P05OC050: Pig enzymes of biotransformation</a><br>

Continuities

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Publication year

2007

Confidentiality

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

Name of the periodical

Biomedical Papers

ISSN

1213-8118

e-ISSN

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Volume of the periodical

151

Issue of the periodical within the volume

S1

Country of publishing house

CZ - CZECH REPUBLIC

Number of pages

2

Pages from-to

53-54

UT code for WoS article

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EID of the result in the Scopus database

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