In vitro reactivation potency of acetylcholinesterase reactivators--K074 and K075--to reactivate tabun-inhibited human brain cholinesterases
Jazyk angličtina Země Spojené státy americké Médium print
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
17449453
DOI
10.1007/bf03033389
Knihovny.cz E-zdroje
- MeSH
- acetylcholinesterasa metabolismus MeSH
- aktivace enzymů účinky léků MeSH
- butany chemie farmakologie MeSH
- cholinesterasové inhibitory toxicita MeSH
- lidé MeSH
- nucleus caudatus účinky léků enzymologie MeSH
- obidoxim chlorid chemie farmakologie MeSH
- organofosfáty toxicita MeSH
- oximy chemie farmakologie MeSH
- pralidoximové sloučeniny chemie farmakologie MeSH
- pyridinové sloučeniny chemie farmakologie MeSH
- reaktivátory cholinesterázy chemie farmakologie MeSH
- techniky in vitro MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1,4-bis(4-hydroxyiminomethylpyridinium)butane dibromide MeSH Prohlížeč
- acetylcholinesterasa MeSH
- asoxime chloride MeSH Prohlížeč
- butany MeSH
- cholinesterasové inhibitory MeSH
- K075 compound MeSH Prohlížeč
- N,N'-monomethylenebis(pyridiniumaldoxime) MeSH Prohlížeč
- obidoxim chlorid MeSH
- organofosfáty MeSH
- oximy MeSH
- pralidoxime MeSH Prohlížeč
- pralidoximové sloučeniny MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterázy MeSH
- tabun MeSH Prohlížeč
In this work, two oximes for the treatment of tabun-inhibited acetylcholinesterase (AChE; EC 3.1.1.7), K074 (1,4-bis(4-hydroxyiminomethylpyridinium)butane dibromide) and K075 ((E)-1,4-bis(4-hydroxyiminomethylpyridinium)but-2-en dibromide), were tested in vitro as reactivators of AChE. Comparison was made with currently used AChE reactivators (pralidoxime, HI-6, methoxime and obidoxime). Human brain homogenate was taken as an appropriate source of the cholinesterases. As resulted, oxime K074 appears to be the most potent reactivator of tabun-inhibited AChE, with reactivation potency comparable to that of obidoxime. A second AChE reactivator, K075, does not attain as great a reactivation potency as K074, although its maximal reactivation (17%) was achieved at relevant concentrations for humans.
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