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Statements

Subject Item
n2:RIV%2F61989592%3A15110%2F07%3A00004264%21RIV08-MSM-15110___
rdf:type
n4:Vysledek skos:Concept
dcterms: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-pass metabolism 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 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-pass metabolism 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 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.
dcterms:title
Interakce nabumetonu s cytochromy P450 in vitro: srovnání u člověka a prasete INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG
skos:prefLabel
Interakce nabumetonu s cytochromy P450 in vitro: srovnání u člověka a prasete INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG
skos:notation
RIV/61989592:15110/07:00004264!RIV08-MSM-15110___
n3:strany
53-54
n3:aktivita
n15:P
n3:aktivity
P(1P05OC050)
n3:cisloPeriodika
S1
n3:dodaniDat
n9:2008
n3:domaciTvurceVysledku
n10:4364058 n10:5975700 n10:7271859 n10:8321124
n3:druhVysledku
n18:J
n3:duvernostUdaju
n11:S
n3:entitaPredkladatele
n12:predkladatel
n3:idSjednocenehoVysledku
427054
n3:idVysledku
RIV/61989592:15110/07:00004264
n3:jazykVysledku
n17:eng
n3:klicovaSlova
Nabumetone; 6-MNA; Cytochrome P450; CYP; Pig
n3:klicoveSlovo
n7:6-MNA n7:Pig n7:Cytochrome%20P450 n7:CYP n7:Nabumetone
n3:kodStatuVydavatele
CZ - Česká republika
n3:kontrolniKodProRIV
[EC7C5F017893]
n3:nazevZdroje
Biomedical Papers
n3:obor
n14:FR
n3:pocetDomacichTvurcuVysledku
4
n3:pocetTvurcuVysledku
5
n3:projekt
n13:1P05OC050
n3:rokUplatneniVysledku
n9:2007
n3:svazekPeriodika
151
n3:tvurceVysledku
Anzenbacherová, Eva Veinlichová, Alena Matal, Jaroslav Anzenbacher, Pavel Nobilis, M.
s:issn
1213-8118
s:numberOfPages
2
n16:organizacniJednotka
15110