Five experimental bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from azinphos-methyl-induced toxicity

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F60162694%3AG44__%2F13%3A43874862" target="_blank" >RIV/60162694:G44__/13:43874862 - isvavai.cz</a>

Výsledek na webu

<a href="http://www.stmconnect.com/sites/default/files/44-50%20%20JEIT-D-12-00009.pdf" target="_blank" >http://www.stmconnect.com/sites/default/files/44-50%20%20JEIT-D-12-00009.pdf</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.7178/jeit.14" target="_blank" >10.7178/jeit.14</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Five experimental bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from azinphos-methyl-induced toxicity

Popis výsledku v původním jazyce

In search of more efficacious treatment options for organophosphate poisoning, several experimental K-oximes have been synthesized, which display excellent in vitro efficacy in protecting acetylcholinesterase from inhibition by a broad variety of organophosphorus compounds. To test the efficacy of these K-oximes (K-27, K-48, K-53, K-74, K-75) in vivo, the extent of oxime-conferred protection from mortality induced by the organophosphate pesticide azinphos-methyl was quantified by Cox survival analysis and compared with that of the clinically available oximes pralidoxime and obidoxime. Rats received azinphos-methyl, which is hepatically converted to the active oxon form, in a dosage of 5, 10 or 15 mýmol, and immediately thereafter intraperitoneal injections of the respective oxime at a dosage of half the LD01. K-53 reduced the relative risk of death (RR) to 0.22 (controls: RR=1; pLESS-THAN OR EQUAL TO0.05), which was significantly (pLESS-THAN OR EQUAL TO0.05) better than obidoxime (RR=0

Název v anglickém jazyce

Five experimental bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from azinphos-methyl-induced toxicity

Popis výsledku anglicky

In search of more efficacious treatment options for organophosphate poisoning, several experimental K-oximes have been synthesized, which display excellent in vitro efficacy in protecting acetylcholinesterase from inhibition by a broad variety of organophosphorus compounds. To test the efficacy of these K-oximes (K-27, K-48, K-53, K-74, K-75) in vivo, the extent of oxime-conferred protection from mortality induced by the organophosphate pesticide azinphos-methyl was quantified by Cox survival analysis and compared with that of the clinically available oximes pralidoxime and obidoxime. Rats received azinphos-methyl, which is hepatically converted to the active oxon form, in a dosage of 5, 10 or 15 mýmol, and immediately thereafter intraperitoneal injections of the respective oxime at a dosage of half the LD01. K-53 reduced the relative risk of death (RR) to 0.22 (controls: RR=1; pLESS-THAN OR EQUAL TO0.05), which was significantly (pLESS-THAN OR EQUAL TO0.05) better than obidoxime (RR=0

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

KA - Vojenství

OECD FORD obor

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Projekt

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Návaznosti

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2013

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název periodika

Journal of Environmental Immunology and Toxicology

ISSN

2225-1219

e-ISSN

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Svazek periodika

1

Číslo periodika v rámci svazku

1

Stát vydavatele periodika

US - Spojené státy americké

Počet stran výsledku

7

Strana od-do

44-50

Kód UT WoS článku

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EID výsledku v databázi Scopus

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