The summary on non-reactivation cholinergic properties of oxime reactivators: the interaction with muscarinic and nicotinic receptors
Language English Country Germany Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't, Review
- MeSH
- Acetylcholinesterase metabolism MeSH
- Antidotes therapeutic use MeSH
- Atropine pharmacology MeSH
- Choline metabolism MeSH
- Cholinergic Antagonists pharmacology MeSH
- Cholinergic Agents pharmacology MeSH
- Cholinesterase Inhibitors metabolism toxicity MeSH
- Inhibitory Concentration 50 MeSH
- Rats MeSH
- Humans MeSH
- Urinary Bladder drug effects metabolism MeSH
- Receptors, Nicotinic drug effects metabolism MeSH
- Organophosphates metabolism toxicity MeSH
- Organophosphate Poisoning drug therapy metabolism MeSH
- Oximes pharmacology MeSH
- Cholinesterase Reactivators pharmacology MeSH
- Receptors, Muscarinic drug effects metabolism MeSH
- Muscle Contraction drug effects MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Humans MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Review MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Antidotes MeSH
- Atropine MeSH
- Choline MeSH
- Cholinergic Antagonists MeSH
- Cholinergic Agents MeSH
- Cholinesterase Inhibitors MeSH
- Receptors, Nicotinic MeSH
- Organophosphates MeSH
- Oximes MeSH
- Cholinesterase Reactivators MeSH
- Receptors, Muscarinic MeSH
Organophosphorus inhibitors (OP) of acetylcholinesterase (AChE) represent a group of highly toxic compounds. The treatment of OP intoxication is, however, insufficiently ensured. Currently, two main categories of drugs-anticholinergics and oxime reactivators- are employed as antidotes. Oximes have been reported to act at several levels of the cholinergic transmission, and among the non-reactivation effects, the interaction with cholinergic receptors stands out. This review addresses issues correlated with non-reactivating effects of oxime reactivators with a special focus on the muscarinic and nicotinic receptors, but involvement of other cholinergic structures such as AChE and choline uptake carriers are discussed too. It can be concluded that the oxime reactivators show a variation in their antagonistic effect on the muscarinic and nicotinic receptors, which is likely to be of significance in the treatment of OP poisoning. In vitro data reported oximes to exert higher efficacy on the muscarinic M2 subtype than on the AChE. However, this effect seemed to be subtype specific since the antagonistic M3 effect was lower. Also, and importantly, the antimuscarinic effect was larger than that on nicotinic receptors. Even though atropine showed a much higher muscarinic antagonism, it is supposed that non-reactivation properties of oxime reactivators play a significant role in the treatment of OP poisoning.
References provided by Crossref.org
A-series agent A-234: initial in vitro and in vivo characterization
A-agents, misleadingly known as "Novichoks": a narrative review
Toxic Injury to Muscle Tissue of Rats Following Acute Oximes Exposure
