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Reactivators of butyrylcholinesterase inhibited by organophosphorus compounds
Z. Kohoutova, E. Prchalova, K. Knittelova, K. Musilek, D. Malinak
Language English Country United States
Document type Journal Article, Review
- MeSH
- Acetylcholinesterase metabolism chemistry MeSH
- Butyrylcholinesterase * metabolism chemistry MeSH
- Cholinesterase Inhibitors * chemistry pharmacology chemical synthesis MeSH
- Humans MeSH
- Molecular Structure MeSH
- Organophosphorus Compounds * chemistry pharmacology MeSH
- Cholinesterase Reactivators pharmacology chemistry chemical synthesis MeSH
- Structure-Activity Relationship MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Review MeSH
In this review, the current progress in the research and development of butyrylcholinesterase (BChE) reactivators is summarised and the advantages or disadvantages of these reactivators are critically discussed. Organophosphorus compounds such as nerve agents (sarin, tabun, VX) or pesticides (chlorpyrifos, diazinon) cause irreversible inhibition of acetylcholinesterase (AChE) and BChE in the human body. While AChE inhibition can be life threatening due to cholinergic overstimulation and crisis, selective BChE inhibition has presumably no adverse effects. Because BChE is mostly found in plasma, its activity is important for the scavenging of organophosphates before they can reach AChE in the central nervous system. Therefore, this enzyme in combination with its reactivator can be used as a pseudo-catalytic scavenger of organophosphates. Three structural types of BChE reactivators were found, i.e. bisquaternary salts, monoquaternary salts and uncharged compounds. Although the reviewed reactivators have certain limitations, the promising candidates for BChE reactivation were found in each structural group.
References provided by Crossref.org
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