The summary on non-reactivation cholinergic properties of oxime reactivators: the interaction with muscarinic and nicotinic receptors
Jazyk angličtina Země Německo Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem, přehledy
- MeSH
- acetylcholinesterasa metabolismus MeSH
- antidota terapeutické užití MeSH
- atropin farmakologie MeSH
- cholin metabolismus MeSH
- cholinergní antagonisté farmakologie MeSH
- cholinergní látky farmakologie MeSH
- cholinesterasové inhibitory metabolismus toxicita MeSH
- inhibiční koncentrace 50 MeSH
- krysa rodu Rattus MeSH
- lidé MeSH
- močový měchýř účinky léků metabolismus MeSH
- nikotinové receptory účinky léků metabolismus MeSH
- organofosfáty metabolismus toxicita MeSH
- otrava organofosfáty farmakoterapie metabolismus MeSH
- oximy farmakologie MeSH
- reaktivátory cholinesterázy farmakologie MeSH
- receptory muskarinové účinky léků metabolismus MeSH
- svalová kontrakce účinky léků MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
- Názvy látek
- acetylcholinesterasa MeSH
- antidota MeSH
- atropin MeSH
- cholin MeSH
- cholinergní antagonisté MeSH
- cholinergní látky MeSH
- cholinesterasové inhibitory MeSH
- nikotinové receptory MeSH
- organofosfáty MeSH
- oximy MeSH
- reaktivátory cholinesterázy MeSH
- receptory muskarinové 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.
Citace poskytuje Crossref.org
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