Butyrylcholinesterase inhibited by nerve agents is efficiently reactivated with chlorinated pyridinium oximes
Jazyk angličtina Země Irsko Médium print-electronic
Typ dokumentu časopisecké články
PubMed
31004594
DOI
10.1016/j.cbi.2019.04.020
PII: S0009-2797(19)30394-1
Knihovny.cz E-zdroje
- Klíčová slova
- Cholinesterase, Organophosphorus compounds, Pseudo-catalytic scavenger, Quaternary oxime, Reactivators,
- MeSH
- aktivace enzymů účinky léků MeSH
- butyrylcholinesterasa chemie metabolismus MeSH
- cholinesterasové inhibitory chemie metabolismus MeSH
- halogenace MeSH
- kinetika MeSH
- lidé MeSH
- nervová bojová látka chemie metabolismus MeSH
- oximy chemie metabolismus farmakologie MeSH
- pyridinové sloučeniny chemie MeSH
- sarin chemie metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- Názvy látek
- butyrylcholinesterasa MeSH
- cholinesterasové inhibitory MeSH
- nervová bojová látka MeSH
- oximy MeSH
- pyridinové sloučeniny MeSH
- sarin MeSH
Bispyridinium oximes with one (K865, K866, K867) or two (K868, K869, K870) ortho-positioned chlorine moiety, analogous to previously known K027, K048 and K203 oximes, and potent reactivators of human acetylcholinesterase (AChE) inhibited by nerve agents, were tested in the reactivation of human butyrylcholinesterase (BChE) inhibited by sarin, cyclosarin, VX, and tabun. A previously highlighted AChE reactivator, dichlorinated bispyridinium oxime with propyl linker (K868), was tested in more detail for reactivation of four nerve agent-BChE conjugates. Its BChE reactivation potency was showed to be promising when compared to the standard oximes used in medical practice, asoxime (HI-6) and pralidoxime (2-PAM), especially in case of sarin and tabun. This finding could be used in the pseudo-catalytic scavenging of the most nerve agents due to its cumulative capacity to reactivate both AChE and BChE.
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