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| Description
| - 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=0.37) or pralidoxime (RR=0.39). Statistically significant reduction in mortality compared to controls was also achieved by all other tested oximes: K-27 (RR=0.26), K-75 (RR=0.27), K-74 (RR=0.31) and K-48 (RR=0.33), but their difference in efficacy did not reach statistical significance, when compared to that of the two established oximes obidoxime and pralidoxime. These in vivo data indicate that K-27 and K-53 are amongst the most promising K-oximes.
- 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=0.37) or pralidoxime (RR=0.39). Statistically significant reduction in mortality compared to controls was also achieved by all other tested oximes: K-27 (RR=0.26), K-75 (RR=0.27), K-74 (RR=0.31) and K-48 (RR=0.33), but their difference in efficacy did not reach statistical significance, when compared to that of the two established oximes obidoxime and pralidoxime. These in vivo data indicate that K-27 and K-53 are amongst the most promising K-oximes. (en)
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| Title
| - Five experimental bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from azinphos-methyl-induced toxicity
- Five experimental bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from azinphos-methyl-induced toxicity (en)
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| skos:prefLabel
| - Five experimental bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from azinphos-methyl-induced toxicity
- Five experimental bispyridinium oximes in comparison with the conventional oximes pralidoxime and obidoxime: in vivo efficacy to protect from azinphos-methyl-induced toxicity (en)
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| skos:notation
| - RIV/60162694:G44__/13:43874862!RIV14-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
| |
| 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
| |
| http://linked.open...ai/riv/idVysledku
| - RIV/60162694:G44__/13:43874862
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| http://linked.open...riv/jazykVysledku
| |
| http://linked.open.../riv/klicovaSlova
| - rat; pesticides; organophosphate; oximes; cox analysis; cholinesterase; azinphos-methyl; acetylcholine (en)
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| http://linked.open.../riv/klicoveSlovo
| |
| http://linked.open...odStatuVydavatele
| - US - Spojené státy americké
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Journal of Environmental Immunology and Toxicology
|
| http://linked.open...in/vavai/riv/obor
| |
| http://linked.open...ichTvurcuVysledku
| |
| http://linked.open...cetTvurcuVysledku
| |
| http://linked.open...UplatneniVysledku
| |
| http://linked.open...v/svazekPeriodika
| |
| http://linked.open...iv/tvurceVysledku
| - Kuča, Kamil
- Hasan, Mohamed Y.
- Lorke, Dietrich E.
- Nurulain, Syed M.
- Petroianu, Georg A.
|
| issn
| |
| number of pages
| |
| http://bibframe.org/vocab/doi
| |
| http://localhost/t...ganizacniJednotka
| |
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