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From pyridinium-based to centrally active acetylcholinesterase reactivators
J. Korabecny, O. Soukup, R. Dolezal, K. Spilovska, E. Nepovimova, M. Andrs, TD. Nguyen, D. Jun, K. Musilek, M. Kucerova-Chlupacova, K. Kuca,
Jazyk angličtina Země Nizozemsko
Typ dokumentu časopisecké články, práce podpořená grantem, přehledy
Grantová podpora
NT12062
MZ0
CEP - Centrální evidence projektů
- MeSH
- acetylcholinesterasa metabolismus MeSH
- lidé MeSH
- objevování léků MeSH
- otrava organofosfáty farmakoterapie MeSH
- pyridinové sloučeniny chemie farmakologie terapeutické užití MeSH
- reaktivátory cholinesterázy chemie farmakologie terapeutické užití MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
Organophosphates are used as pesticides or misused as warfare nerve agents. Exposure to them can be fatal and death is usually caused by respiratory arrest. For almost six decades, pyridinium oximes represent a therapeutic tool used for the management of poisoning with organophosphorus (OP) compounds. However, these compounds possess several drawbacks. Firstly, they are inefficient in the restoration of brain acetylcholinesterase (AChE) activity due to a hard blood-brain barrier penetration. Secondly, there is no broad-spectrum AChE reactivator. Lastly, none of the oximes can reactivate "aged" AChE. In this context, uncharged reactivators represent a new hope in a way of increased bioavailability in the central compartment and better therapeutic management of the OP poisoning.
Citace poskytuje Crossref.org
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- $a Organophosphates are used as pesticides or misused as warfare nerve agents. Exposure to them can be fatal and death is usually caused by respiratory arrest. For almost six decades, pyridinium oximes represent a therapeutic tool used for the management of poisoning with organophosphorus (OP) compounds. However, these compounds possess several drawbacks. Firstly, they are inefficient in the restoration of brain acetylcholinesterase (AChE) activity due to a hard blood-brain barrier penetration. Secondly, there is no broad-spectrum AChE reactivator. Lastly, none of the oximes can reactivate "aged" AChE. In this context, uncharged reactivators represent a new hope in a way of increased bioavailability in the central compartment and better therapeutic management of the OP poisoning.
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