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Statements

Subject Item
n2:RIV%2F60162694%3AG44__%2F09%3A00002423%21RIV11-MO0-G44_____
rdf:type
skos:Concept n15:Vysledek
dcterms:description
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.
dcterms:title
Evaluation of oxime K203 as antidote in tabun poisoning Evaluation of oxime K203 as antidote in tabun poisoning
skos:prefLabel
Evaluation of oxime K203 as antidote in tabun poisoning Evaluation of oxime K203 as antidote in tabun poisoning
skos:notation
RIV/60162694:G44__/09:00002423!RIV11-MO0-G44_____
n3:aktivita
n12:N
n3:aktivity
N
n3:cisloPeriodika
1
n3:dodaniDat
n10:2011
n3:domaciTvurceVysledku
n7:6469922 n7:6306888
n3:druhVysledku
n11:J
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n13:predkladatel
n3:idSjednocenehoVysledku
313895
n3:idVysledku
RIV/60162694:G44__/09:00002423
n3:jazykVysledku
n8:eng
n3:klicovaSlova
acetylcholinesterase; bioscavenger; butyrylcholinesterase; K048; nerve agents; TMB-4; pyridinium oxime
n3:klicoveSlovo
n5:pyridinium%20oxime n5:acetylcholinesterase n5:K048 n5:TMB-4 n5:nerve%20agents n5:bioscavenger n5:butyrylcholinesterase
n3:kodStatuVydavatele
HR - Chorvatská republika
n3:kontrolniKodProRIV
[D0C2D4B02747]
n3:nazevZdroje
Archives of Industrial Hygiene and Toxicology
n3:obor
n14:FP
n3:pocetDomacichTvurcuVysledku
2
n3:pocetTvurcuVysledku
7
n3:rokUplatneniVysledku
n10:2009
n3:svazekPeriodika
60
n3:tvurceVysledku
Musílek, Kamil Berend, S. Radic, B. Kovarik, Zrinka Lucic Vrdoljak, A. Calic, M. Kuča, Kamil
s:issn
0004-1254
s:numberOfPages
8
n16:organizacniJednotka
G44