About: Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium-oximes     Goto   Sponge   NotDistinct   Permalink

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Description
  • Cyclohexyl methylphosphonofluoridate (cyclosarin, cyclosin, GF) is a highly toxic organophosphate, which was resistant to conventional oxime therapy. To give more insight into the reactivation kinetics, rat brain acetylcholinesterase (AChE) was inhibited in vitro by cyclosarin (pH 8.0, 25 °C) and reactivated with 22 different pyridinium-oximes. Only three compounds were shown to be superior to the other oximes: 4-carbamoyl-4´-[(hydroxyimino)methyl]-1,1´-(oxydimethylene)dipyridin-1-ium dichloride (HS-6), 4´-carbamoyl-2-[(hydroxyimino)methyl]-1,1´-(oxydimethylene)dipyridin-1-ium dichloride (HI-6), and 4´-carbamoyl-2-[(hydroxyimino)methyl]-1,1´-(but-2-ene-1,4-diyl)dipyridin-1-ium dichloride (BI-6).
  • Cyclohexyl methylphosphonofluoridate (cyclosarin, cyclosin, GF) is a highly toxic organophosphate, which was resistant to conventional oxime therapy. To give more insight into the reactivation kinetics, rat brain acetylcholinesterase (AChE) was inhibited in vitro by cyclosarin (pH 8.0, 25 °C) and reactivated with 22 different pyridinium-oximes. Only three compounds were shown to be superior to the other oximes: 4-carbamoyl-4´-[(hydroxyimino)methyl]-1,1´-(oxydimethylene)dipyridin-1-ium dichloride (HS-6), 4´-carbamoyl-2-[(hydroxyimino)methyl]-1,1´-(oxydimethylene)dipyridin-1-ium dichloride (HI-6), and 4´-carbamoyl-2-[(hydroxyimino)methyl]-1,1´-(but-2-ene-1,4-diyl)dipyridin-1-ium dichloride (BI-6). (en)
  • Reaktivace cyklosarinem inhibované acetylcholinesterázy pyridiniovými oximy (cs)
Title
  • Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium-oximes
  • Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium-oximes (en)
  • Reaktivace cyklosarinem inhibované acetylcholinesterázy pyridiniovými oximy (cs)
skos:prefLabel
  • Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium-oximes
  • Reactivation of cyclosarin-inhibited rat brain acetylcholinesterase by pyridinium-oximes (en)
  • Reaktivace cyklosarinem inhibované acetylcholinesterázy pyridiniovými oximy (cs)
skos:notation
  • RIV/60162694:G38__/04:00001080!RIV/2005/MO0/G38005/N
http://linked.open.../vavai/riv/strany
  • 39-43
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(ONVLAJEP20031)
http://linked.open...iv/cisloPeriodika
  • 1
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
  • 583624
http://linked.open...ai/riv/idVysledku
  • RIV/60162694:G38__/04:00001080
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • acetylcholinesterase;oxime;reactivation;cyclosarin;in vitro (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [C4B9E30C731A]
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...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 19
http://linked.open...iv/tvurceVysledku
  • Kuča, Kamil
  • Patočka, Jiří
issn
  • 8755-5093
number of pages
http://localhost/t...ganizacniJednotka
  • G38
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