From pyridinium-based to centrally active acetylcholinesterase reactivators
Language English Country Netherlands Media print
Document type Journal Article, Research Support, Non-U.S. Gov't, Review
PubMed
24552265
DOI
10.2174/1389557514666140219103138
PII: MRMC-EPUB-59253
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase metabolism MeSH
- Humans MeSH
- Drug Discovery MeSH
- Organophosphate Poisoning drug therapy MeSH
- Pyridinium Compounds chemistry pharmacology therapeutic use MeSH
- Cholinesterase Reactivators chemistry pharmacology therapeutic use MeSH
- Animals MeSH
- Check Tag
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Review MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators 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.
References provided by Crossref.org
Acute Toxic Injuries of Rat's Visceral Tissues Induced by Different Oximes
Novichoks: The Dangerous Fourth Generation of Chemical Weapons
Toxic Injury to Muscle Tissue of Rats Following Acute Oximes Exposure
Synthesis and disinfection effect of the pyridine-4-aldoxime based salts