Slow-binding reversible inhibitor of acetylcholinesterase with long-lasting action for prophylaxis of organophosphate poisoning.
Animals
Benzylammonium Compounds
/ administration & dosage
Bromides
/ administration & dosage
Cholinesterase Inhibitors
/ administration & dosage
Delayed-Action Preparations
Disease Models, Animal
Mice
Organophosphate Poisoning
/ prevention & control
Organophosphorus Compounds
/ toxicity
Paraoxon
/ toxicity
Pyridostigmine Bromide
/ administration & dosage
Time Factors
Journal
Scientific reports
ISSN: 2045-2322
Titre abrégé: Sci Rep
Pays: England
ID NLM: 101563288
Informations de publication
Date de publication:
06 10 2020
06 10 2020
Historique:
received:
29
07
2020
accepted:
22
09
2020
entrez:
7
10
2020
pubmed:
8
10
2020
medline:
11
3
2021
Statut:
epublish
Résumé
Organophosphorus (OP) compounds represent a serious health hazard worldwide. The dominant mechanism of their action results from covalent inhibition of acetylcholinesterase (AChE). Standard therapy of acute OP poisoning is partially effective. However, prophylactic administration of reversible or pseudo-irreversible AChE inhibitors before OP exposure increases the efficiency of standard therapy. The purpose of the study was to test the duration of the protective effect of a slow-binding reversible AChE inhibitor (C547) in a mouse model against acute exposure to paraoxon (POX). It was shown that the rate of inhibition of AChE by POX in vitro after pre-inhibition with C547 was several times lower than without C547. Ex vivo pre-incubation of mouse diaphragm with C547 significantly prevented the POX-induced muscle weakness. Then it was shown that pre-treatment of mice with C547 at the dose of 0.01 mg/kg significantly increased survival after poisoning by 2xLD
Identifiants
pubmed: 33024231
doi: 10.1038/s41598-020-73822-6
pii: 10.1038/s41598-020-73822-6
pmc: PMC7538863
doi:
Substances chimiques
AChE inhibitor C547
0
Benzylammonium Compounds
0
Bromides
0
Cholinesterase Inhibitors
0
Delayed-Action Preparations
0
Organophosphorus Compounds
0
Pyridostigmine Bromide
KVI301NA53
Paraoxon
Q9CX8P80JW
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
16611Références
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