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  • Organophosphate compounds exert toxicity primarily by virtue of acetylcholinesterase (AChE) inactivation at the nerve synapses and neuromuscular junction, leading to accumulation of acetylcholine (ACh). Therefore, treatment of organophosphate poisonings generally relies upon AChE reactivators, anticholinergic drugs, and anticonvulsants. Although there are many structurally different AChE reactivators, only five of them are used clinically. Unfortunately, there is not a single compound that can reactivate inhibited AChE against all nerve agents, or a so-called broad spectrum reactivator. Due to this limitation, the quest for new derivatives continues. For newly synthesized derivatives, in vitro and in vivo evaluation of their reactivation efficacy is of the utmost importance in AChE reactivators' development. This review article presents literature on the most promising novel AChE reactivators. Furthermore, in vitro and in vivo techniques used for their evaluation are also discussed.
  • Organophosphate compounds exert toxicity primarily by virtue of acetylcholinesterase (AChE) inactivation at the nerve synapses and neuromuscular junction, leading to accumulation of acetylcholine (ACh). Therefore, treatment of organophosphate poisonings generally relies upon AChE reactivators, anticholinergic drugs, and anticonvulsants. Although there are many structurally different AChE reactivators, only five of them are used clinically. Unfortunately, there is not a single compound that can reactivate inhibited AChE against all nerve agents, or a so-called broad spectrum reactivator. Due to this limitation, the quest for new derivatives continues. For newly synthesized derivatives, in vitro and in vivo evaluation of their reactivation efficacy is of the utmost importance in AChE reactivators' development. This review article presents literature on the most promising novel AChE reactivators. Furthermore, in vitro and in vivo techniques used for their evaluation are also discussed. (en)
Title
  • In vitro identification of novel acetylcholinesterase reactivators
  • In vitro identification of novel acetylcholinesterase reactivators (en)
skos:prefLabel
  • In vitro identification of novel acetylcholinesterase reactivators
  • In vitro identification of novel acetylcholinesterase reactivators (en)
skos:notation
  • RIV/60162694:G44__/09:00002214!RIV10-GA0-G44_____
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GP305/07/P162), S
http://linked.open...iv/cisloPeriodika
  • 4
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
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  • 318919
http://linked.open...ai/riv/idVysledku
  • RIV/60162694:G44__/09:00002214
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  • acetylcholinesterase; nerve agents; organophosphorus inhibitors; oxime; reactivator (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [700B0A47BBE2]
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  • Toxin Reviews
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http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 28
http://linked.open...iv/tvurceVysledku
  • Kuča, Kamil
  • Musílek, Kamil
  • Pohanka, Miroslav
  • Jun, Daniel
  • Gupta, R. C.
http://linked.open...ain/vavai/riv/wos
  • 000273048000002
issn
  • 1556-9543
number of pages
http://localhost/t...ganizacniJednotka
  • G44
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