About: In vitro and in vivo evaluation of pyridinium oximes: mode of interaction with acetylcholinesterase, effect on tabun- and soman-poisoned mice and their cytotoxicity     Goto   Sponge   NotDistinct   Permalink

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  • Byly sledovány in vitro a in vivo interakce pyridiniových oximů (K027, K048, K033, TMB-4 a HI-6) s enzymem acetylcholinesterázou a dále účinek těchto látek u myší intoxikovaných nervově paralytickými látkami tabun a soman. Dále byla testována cytotoxicita uvedených látek. (cs)
  • The increased concern about terrorist use of nerve agents prompted us to search for new more effective oximes against tabun and soman poisoning. We investigated the interactions of five bispyridinium oximes: K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium) propane dibromide], K048 [1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium) butane dibromide], K033 [1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide], TMB-4 [1,3-bis(4-hydroxyiminomethylpyridinium) propane dibromide] and HI-6 [(1-(2-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-2-oxapropane dichloride)] with human erythrocyte acetylcholinesterase (AChE; E.C. 3.1.1.7) and their effects on tabun- and soman-poisoned mice. All the oximes reversibly inhibited AChE, and the enzyme-oxime dissociation constants were between 17 and 180 microM. Tabun-inhibited AChE was completely reactivated by TMB-4, K027 and K048, with the overall reactivation rate constants of 306, 376 and 673 min(-1)M(-1), respectively. The
  • The increased concern about terrorist use of nerve agents prompted us to search for new more effective oximes against tabun and soman poisoning. We investigated the interactions of five bispyridinium oximes: K027 [1-(4-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium) propane dibromide], K048 [1-(4-hydroxyiminomethylpyridinium)-4-(4-carbamoylpyridinium) butane dibromide], K033 [1,4-bis(2-hydroxyiminomethylpyridinium) butane dibromide], TMB-4 [1,3-bis(4-hydroxyiminomethylpyridinium) propane dibromide] and HI-6 [(1-(2-hydroxyiminomethylpyridinium)-3-(4-carbamoylpyridinium)-2-oxapropane dichloride)] with human erythrocyte acetylcholinesterase (AChE; E.C. 3.1.1.7) and their effects on tabun- and soman-poisoned mice. All the oximes reversibly inhibited AChE, and the enzyme-oxime dissociation constants were between 17 and 180 microM. Tabun-inhibited AChE was completely reactivated by TMB-4, K027 and K048, with the overall reactivation rate constants of 306, 376 and 673 min(-1)M(-1), respectively. The (en)
Title
  • In vitro a in vivo hodnocení pyridiniových oximů: způsob jejich interakce s acetylcholinesterázou, jejich účinek u myší intoxikovaných tabunem a somanem a jejich cytotoxicita (cs)
  • In vitro and in vivo evaluation of pyridinium oximes: mode of interaction with acetylcholinesterase, effect on tabun- and soman-poisoned mice and their cytotoxicity
  • In vitro and in vivo evaluation of pyridinium oximes: mode of interaction with acetylcholinesterase, effect on tabun- and soman-poisoned mice and their cytotoxicity (en)
skos:prefLabel
  • In vitro a in vivo hodnocení pyridiniových oximů: způsob jejich interakce s acetylcholinesterázou, jejich účinek u myší intoxikovaných tabunem a somanem a jejich cytotoxicita (cs)
  • In vitro and in vivo evaluation of pyridinium oximes: mode of interaction with acetylcholinesterase, effect on tabun- and soman-poisoned mice and their cytotoxicity
  • In vitro and in vivo evaluation of pyridinium oximes: mode of interaction with acetylcholinesterase, effect on tabun- and soman-poisoned mice and their cytotoxicity (en)
skos:notation
  • RIV/60162694:G44__/06:00001476!RIV09-MO0-G44_____
http://linked.open...avai/riv/aktivita
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  • Z(MO0FVZ0000501)
http://linked.open...iv/cisloPeriodika
  • 1-3
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 479131
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  • RIV/60162694:G44__/06:00001476
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  • acetylcholinesterase; antidote; nerve agent; inhibition; reactivation; oxime; antidotal treatment (en)
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  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [30E435055E88]
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  • Toxicology
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  • 219
http://linked.open...iv/tvurceVysledku
  • Kuča, Kamil
  • Jun, Daniel
  • Kovarik, Z.
  • Lucic Vrdoljak, A.
  • Jelic, D.
  • Radić, B.
  • Čalić, M.
http://linked.open...n/vavai/riv/zamer
issn
  • 0300-483X
number of pages
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  • G44
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