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| Description
| - Oximes are enzyme reactivators used in treating poisoning with organophosphorus cholinesterase (AChE) inhibitors. The oxime dose which can be safely administered is limited by the intrinsic toxicity of the substances such as their own AChE-inhibiting tendency. Clinical experience with the available oximes is disappointing. To meet this need, new AChE reactivators of potential clinical utility have been developed. The purpose of the study was to estimate in vitro both the intrinsic toxicity and the extent of possible protection conferred by established (pralidoxime, obidoxime, HI-6, methoxime, trimedoxime) and experimental (K-type) oximes, using diisopropyl-fluoro-phosphate (DFP) as an AChE inhibitor. The IC50 of DFP against human red blood cell AChE was determined (~120 nM). Measurements were then repeated in the presence of increasing oxime concentrations, leading to an apparent increase in DFP IC50. Calculated IC50 values were plotted against oxime concentrations to obtain an IC50 shift curve. The s
- Oximes are enzyme reactivators used in treating poisoning with organophosphorus cholinesterase (AChE) inhibitors. The oxime dose which can be safely administered is limited by the intrinsic toxicity of the substances such as their own AChE-inhibiting tendency. Clinical experience with the available oximes is disappointing. To meet this need, new AChE reactivators of potential clinical utility have been developed. The purpose of the study was to estimate in vitro both the intrinsic toxicity and the extent of possible protection conferred by established (pralidoxime, obidoxime, HI-6, methoxime, trimedoxime) and experimental (K-type) oximes, using diisopropyl-fluoro-phosphate (DFP) as an AChE inhibitor. The IC50 of DFP against human red blood cell AChE was determined (~120 nM). Measurements were then repeated in the presence of increasing oxime concentrations, leading to an apparent increase in DFP IC50. Calculated IC50 values were plotted against oxime concentrations to obtain an IC50 shift curve. The s (en)
- Oximy jsou enzymové reaktivátory užívané v léčbě otrav organofosforovými cholinesterázovými (AChE) inhibitory. Oximová dávka , která může být bezpečně podána je limitována vlastní toxicitou sloučenin jako vlastní AChE-inhibující tendencí. Clinické zkušenosti s dostupnými oximy jsou špatné. Za tímto účelem se vyvíjejí nové reaktivátory pro clinickou praxi. Účelem této práce bylo zhodnotit in vitro oboje - vlastní toxicitu a míru možné protekce porovnanou s pralidoximem, obidoximem, HI-6, methoximem, trimedoximem a experimentálními K-typy oximů, užitím DFP jako inhibitoru AChE. IC50 DFP vůči krevní AChE byla určena - 120 mM. Měření byly následně zopakovány v přítomnosti vzrůstající oximové koncentrace, vedoucí k zjevnému zvýšení IC50 DFP. Spočítané hodnoty IC50 byly zakreslen oproti oximové koncentraci za účelem posunu křivky IC50. Sklon posunu této křivky (tan) byl užit ke kvntifikaci maxima protektivního efektu (nM IC50 vzůst per mikroM oximu). Ukázali jsme že vazebná konstanta K určená Schildovou rov (cs)
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| Title
| - In vitro oxime protection of human red blood cell acetylcholinesterase inhibited by diisopropyl-fluorophosphate
- In vitro oxime protection of human red blood cell acetylcholinesterase inhibited by diisopropyl-fluorophosphate (en)
- In vitro oximová protekce lidské krevní acetylcholinesterazy inhibované DFP (cs)
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| skos:prefLabel
| - In vitro oxime protection of human red blood cell acetylcholinesterase inhibited by diisopropyl-fluorophosphate
- In vitro oxime protection of human red blood cell acetylcholinesterase inhibited by diisopropyl-fluorophosphate (en)
- In vitro oximová protekce lidské krevní acetylcholinesterazy inhibované DFP (cs)
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| skos:notation
| - RIV/60162694:G44__/08:00001925!RIV09-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__/08:00001925
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - organophosphate; cholinesterase; DFP; oxime; K-oximes; Schild equation (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
| - GB - Spojené království Velké Británie a Severního Irska
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Journal of Applied 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
- Schmitt, A.
- Petroianu, G. A.
- Hasan, M. Y.
- Lorke, D. E.
- Arafat, K.
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| http://linked.open...ain/vavai/riv/wos
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| http://linked.open...n/vavai/riv/zamer
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| issn
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| number of pages
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| http://localhost/t...ganizacniJednotka
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| is http://linked.open...avai/riv/vysledek
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