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| 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. (en)
- 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. (cs)
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| Title
| - New bispyridinium oximes: in vitro evaluation of their biochemical parameters
- Nové bispyridiniové oximy: in vitro zhodnocení jejich biochemických parametrů (cs)
- New bispyridinium oximes: in vitro evaluation of their biochemical parameters (en)
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| skos:prefLabel
| - New bispyridinium oximes: in vitro evaluation of their biochemical parameters
- Nové bispyridiniové oximy: in vitro zhodnocení jejich biochemických parametrů (cs)
- New bispyridinium oximes: in vitro evaluation of their biochemical parameters (en)
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| skos:notation
| - RIV/60162694:G44__/08:00001923!RIV09-MO0-G44_____
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| http://linked.open...avai/riv/aktivita
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| http://linked.open...avai/riv/aktivity
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| http://linked.open...iv/cisloPeriodika
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| http://linked.open...vai/riv/dodaniDat
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| http://linked.open...aciTvurceVysledku
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| http://linked.open.../riv/druhVysledku
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| http://linked.open...iv/duvernostUdaju
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| http://linked.open...titaPredkladatele
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| http://linked.open...dnocenehoVysledku
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| http://linked.open...ai/riv/idVysledku
| - RIV/60162694:G44__/08:00001923
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - oxime; reactivator; nerve agent; acetylcholinesterase; soman; tabun (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Chemico-Biological Interactions
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| http://linked.open...in/vavai/riv/obor
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| http://linked.open...ichTvurcuVysledku
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| http://linked.open...cetTvurcuVysledku
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| http://linked.open...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Kuča, Kamil
- Berend, S.
- Radic, B.
- Lucic Vrdoljak, A.
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| http://linked.open...ain/vavai/riv/wos
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| http://linked.open...n/vavai/riv/zamer
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| issn
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| number of pages
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| http://localhost/t...ganizacniJednotka
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| is http://linked.open...avai/riv/vysledek
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