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Statements

Subject Item
n2:RIV%2F60162694%3AG44__%2F08%3A00001923%21RIV09-MO0-G44_____
rdf:type
skos:Concept n15:Vysledek
dcterms:description
Improving the efficacy of antidotal treatment of poisonings with nerve agents is still a challenge for the scientific community. This study investigated the interactions of four bispyridinium oximes with human erythrocyte acetylcholinesterase (AChE) and their effects on soman- and tabun-poisoned mice. Oximes HI-6 and TMB-4 were used for comparison.These oximes inhibited AchE with inhibitory potency (IC50) ranging from 0.02 to 1.0 mM. The best reactivating potency (%R) was obtained with K074, when AChE was inhibited by tabun.The protective potency (P50) of all oximes in human erythrocyte AChE inhibited by soman and tabun could not be determined. In tabun-poisoned mice very good antidotal efficacy was obtained with K027, K048, and K074, which makes them interesting for future investigation. The combination of HI-6 and atropine is the therapy of choice for soman poisoning. Improving the efficacy of antidotal treatment of poisonings with nerve agents is still a challenge for the scientific community. This study investigated the interactions of four bispyridinium oximes with human erythrocyte acetylcholinesterase (AChE) and their effects on soman- and tabun-poisoned mice. Oximes HI-6 and TMB-4 were used for comparison.These oximes inhibited AchE with inhibitory potency (IC50) ranging from 0.02 to 1.0 mM. The best reactivating potency (%R) was obtained with K074, when AChE was inhibited by tabun.The protective potency (P50) of all oximes in human erythrocyte AChE inhibited by soman and tabun could not be determined. In tabun-poisoned mice very good antidotal efficacy was obtained with K027, K048, and K074, which makes them interesting for future investigation. The combination of HI-6 and atropine is the therapy of choice for soman poisoning. Vylepšení účinnosti antidotní terapie otrav nervově paralytickými látkami je stále výzvou pro vědeckou komunitu. Tato studie se zabývá interakcemi čtyřech bispyridiniových oximů s lidskou erythrocytární AChE a jejich efekt na somanem a tabunem otrávené myši. Oximy HI-6 a TMB-4 byly užity pro srovnání. Tyto oximy inhibovaly AChE s inhibiční účinností (IC50) od 0.02 do 1.0 mM. Nejlepší reaktivační účinnost (%) dosáhl oxim K074, když byla AChE inhibovaná tabunem. Reaktivační účinnost (P50) všech oximů na erythrocytární lidské AChE inhibované somanem a tabunem nemohla být určena. U tabunem otrávených myší byla dosažena velmi dobrá reaktivační schopnost u látek K027, K048 a K074. Tento výsledek je dělá ajímavými pro další výzkum. Kombinece HI-6 a atropin je vhodnou terapií pro otravy somanem.
dcterms:title
New bispyridinium oximes: in vitro evaluation of their biochemical parameters New bispyridinium oximes: in vitro evaluation of their biochemical parameters Nové bispyridiniové oximy: in vitro zhodnocení jejich biochemických parametrů
skos:prefLabel
New bispyridinium oximes: in vitro evaluation of their biochemical parameters New bispyridinium oximes: in vitro evaluation of their biochemical parameters Nové bispyridiniové oximy: in vitro zhodnocení jejich biochemických parametrů
skos:notation
RIV/60162694:G44__/08:00001923!RIV09-MO0-G44_____
n3:aktivita
n16:Z
n3:aktivity
Z(MO0FVZ0000604)
n3:cisloPeriodika
1-3
n3:dodaniDat
n14:2009
n3:domaciTvurceVysledku
n7:6306888
n3:druhVysledku
n18:J
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n13:predkladatel
n3:idSjednocenehoVysledku
382508
n3:idVysledku
RIV/60162694:G44__/08:00001923
n3:jazykVysledku
n12:eng
n3:klicovaSlova
oxime; reactivator; nerve agent; acetylcholinesterase; soman; tabun
n3:klicoveSlovo
n8:reactivator n8:acetylcholinesterase n8:tabun n8:oxime n8:soman n8:nerve%20agent
n3:kodStatuVydavatele
IE - Irsko
n3:kontrolniKodProRIV
[4067CC1F9E28]
n3:nazevZdroje
Chemico-Biological Interactions
n3:obor
n4:FP
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
4
n3:rokUplatneniVysledku
n14:2008
n3:svazekPeriodika
175
n3:tvurceVysledku
Radic, B. Berend, S. Lucic Vrdoljak, A. Kuča, Kamil
n3:wos
000260110500079
n3:zamer
n9:MO0FVZ0000604
s:issn
0009-2797
s:numberOfPages
4
n10:organizacniJednotka
G44