About: Potency of new structurally different oximes to reactivate cyclosarin inhibited-human brain acetylcholinesterases     Goto   Sponge   NotDistinct   Permalink

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Description
  • Antidotes currently used in the case of organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Owing to the wide-spread of these compounds worldwide, development of antidotes for the case of the first aid is needed. To select the most promising AChE reactivators is very time consuming process, which is necessary before approval of these compounds to be used as human antidotes. Because of ethical reasons, many developing experiments have been conducted on laboratory animals. However, these results could not be often transferred directly to human. Due to this fact, in our work, we have tested five newly developed AChE reactivators # K027, K033, K048, K074 and K075, which achieved promising reactivation activity on rodents, as reactivators of human brain cholinesterases. For this purpose, cyclosarin was used as member of the nerve agent family. H-oxime HI-6 and pralidoxime were used as
  • Antidotes currently used in the case of organophosphorus pesticide and nerve agent intoxications consist of anticholinergics (atropine mainly) and acetylcholinesterase (AChE, EC 3.1.1.7) reactivators called oximes. Owing to the wide-spread of these compounds worldwide, development of antidotes for the case of the first aid is needed. To select the most promising AChE reactivators is very time consuming process, which is necessary before approval of these compounds to be used as human antidotes. Because of ethical reasons, many developing experiments have been conducted on laboratory animals. However, these results could not be often transferred directly to human. Due to this fact, in our work, we have tested five newly developed AChE reactivators # K027, K033, K048, K074 and K075, which achieved promising reactivation activity on rodents, as reactivators of human brain cholinesterases. For this purpose, cyclosarin was used as member of the nerve agent family. H-oxime HI-6 and pralidoxime were used as (en)
  • Schopnost nově vyvinuých reaktivátorů acetylcholinesterázy (K027, K033, K048, K074 a K075) byla testována na cholinesterázách lidského mozku inhibovaných nervově paralytickou látkou cyklosarin. (cs)
Title
  • Potency of new structurally different oximes to reactivate cyclosarin inhibited-human brain acetylcholinesterases
  • Potency of new structurally different oximes to reactivate cyclosarin inhibited-human brain acetylcholinesterases (en)
  • Schopnost nových strukturně odlišných oximů reaktivovat cyclosarinem inhibovanou acetylcholinesterázu z lidského mozku (cs)
skos:prefLabel
  • Potency of new structurally different oximes to reactivate cyclosarin inhibited-human brain acetylcholinesterases
  • Potency of new structurally different oximes to reactivate cyclosarin inhibited-human brain acetylcholinesterases (en)
  • Schopnost nových strukturně odlišných oximů reaktivovat cyclosarinem inhibovanou acetylcholinesterázu z lidského mozku (cs)
skos:notation
  • RIV/60162694:G44__/06:00001490!RIV07-MO0-G44_____
http://linked.open.../vavai/riv/strany
  • 663-666
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • Z(MO0FVZ0000501)
http://linked.open...iv/cisloPeriodika
  • 6
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
  • 493375
http://linked.open...ai/riv/idVysledku
  • RIV/60162694:G44__/06:00001490
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • cholinesterase; reactivator; cyclosarin; human brain; nerve agent (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [6A0CC4783224]
http://linked.open...i/riv/nazevZdroje
  • Journal of Enzyme Inhibition and Medicinal Chemistry
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...iv/tvurceVysledku
  • Bajgar, Jiří
  • Cabal, Jiří
  • Hrabinová, Martina
  • Kuča, Kamil
  • Jun, Daniel
http://linked.open...n/vavai/riv/zamer
issn
  • 1475-6366
number of pages
http://localhost/t...ganizacniJednotka
  • G44
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