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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. (cs)
  • 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 (en)
Title
  • INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG
  • Interakce nabumetonu s cytochromy P450 in vitro: srovnání u člověka a prasete (cs)
  • INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG (en)
skos:prefLabel
  • INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG
  • Interakce nabumetonu s cytochromy P450 in vitro: srovnání u člověka a prasete (cs)
  • INTERACTION OF NABUMETONE WITH CYTOCHROMES P450 IN VITRO:COMPARISON OF THE MAN AND PIG (en)
skos:notation
  • RIV/61989592:15110/07:00004264!RIV08-MSM-15110___
http://linked.open.../vavai/riv/strany
  • 53-54
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(1P05OC050)
http://linked.open...iv/cisloPeriodika
  • S1
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 427054
http://linked.open...ai/riv/idVysledku
  • RIV/61989592:15110/07:00004264
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Nabumetone; 6-MNA; Cytochrome P450; CYP; Pig (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • CZ - Česká republika
http://linked.open...ontrolniKodProRIV
  • [EC7C5F017893]
http://linked.open...i/riv/nazevZdroje
  • Biomedical Papers
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 151
http://linked.open...iv/tvurceVysledku
  • Anzenbacher, Pavel
  • Anzenbacherová, Eva
  • Matal, Jaroslav
  • Nobilis, M.
  • Veinlichová, Alena
issn
  • 1213-8118
number of pages
http://localhost/t...ganizacniJednotka
  • 15110
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