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| - We studied bispyridinium oxime K203 with tabun-inhibited human AChE and BChE in vitro, and its antidotal effect on tabun-poisoned mice and rats in vivo. We compared it with oximes K048 and TMB-4, which have proven the most efficient oxime antidotes in tabun poisoning by now. Tabun-inhibited AChE was completely reactivated by K203, with the overall reactivation rate constant of 1806 L mol(-1) min(-1). This means that K203 is a very potent reactivator of tabun-inhibited AChE. In addition, K203 reversibly inhibited AChE (Ki = 0.090 mmol L(-1)) and BChE (K(i) = 0.91 mmol L(-1)), and exhibited its protective effect against phosphorylation of AChE by tabun in vitro. In vivo, a quarter of the LD50 K203 dose insured survival of all mice after the application of as many as 8 LD50 doses of tabun, which is the highest dosage obtained compared to K048 and TMB-4. This therapeutic improvement obtained by K203 in tabun-poisoning places this oxime in the spotlight for further development.
- We studied bispyridinium oxime K203 with tabun-inhibited human AChE and BChE in vitro, and its antidotal effect on tabun-poisoned mice and rats in vivo. We compared it with oximes K048 and TMB-4, which have proven the most efficient oxime antidotes in tabun poisoning by now. Tabun-inhibited AChE was completely reactivated by K203, with the overall reactivation rate constant of 1806 L mol(-1) min(-1). This means that K203 is a very potent reactivator of tabun-inhibited AChE. In addition, K203 reversibly inhibited AChE (Ki = 0.090 mmol L(-1)) and BChE (K(i) = 0.91 mmol L(-1)), and exhibited its protective effect against phosphorylation of AChE by tabun in vitro. In vivo, a quarter of the LD50 K203 dose insured survival of all mice after the application of as many as 8 LD50 doses of tabun, which is the highest dosage obtained compared to K048 and TMB-4. This therapeutic improvement obtained by K203 in tabun-poisoning places this oxime in the spotlight for further development. (en)
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Title
| - Evaluation of oxime K203 as antidote in tabun poisoning
- Evaluation of oxime K203 as antidote in tabun poisoning (en)
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skos:prefLabel
| - Evaluation of oxime K203 as antidote in tabun poisoning
- Evaluation of oxime K203 as antidote in tabun poisoning (en)
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skos:notation
| - RIV/60162694:G44__/09:00002423!RIV11-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__/09:00002423
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - acetylcholinesterase; bioscavenger; butyrylcholinesterase; K048; nerve agents; TMB-4; pyridinium oxime (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - HR - Chorvatská republika
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Archives of Industrial Hygiene and Toxicology
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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
- Musílek, Kamil
- Berend, S.
- Radic, B.
- Kovarik, Zrinka
- Calic, M.
- Lucic Vrdoljak, A.
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