Symmetrical Bispyridinium Compounds Act as Open Channel Blockers of Cation-Selective Ion Channels.
Journal
ACS pharmacology & translational science
ISSN: 2575-9108
Titre abrégé: ACS Pharmacol Transl Sci
Pays: United States
ID NLM: 101721411
Informations de publication
Date de publication:
08 Mar 2024
08 Mar 2024
Historique:
received:
31
10
2023
revised:
12
01
2024
accepted:
16
01
2024
pmc-release:
15
02
2025
medline:
18
3
2024
pubmed:
18
3
2024
entrez:
18
3
2024
Statut:
epublish
Résumé
Current treatments against organophosphate poisoning (OPP) do not directly address effects mediated by the overstimulation of nicotinic acetylcholine receptors (nAChR). Non-oxime bispyridinium compounds (BPC) promote acetylcholine esterase-independent recovery of organophosphate-induced paralysis. Here, we test the hypothesis that they act by positive modulatory action on nAChRs. Using two-electrode voltage clamp analysis in combination with mutagenesis and molecular docking analysis, the potency and molecular mode of action of a series of nine BPCs was investigated on human α7 and muscle-type nAChRs expressed in
Identifiants
pubmed: 38495220
doi: 10.1021/acsptsci.3c00308
pmc: PMC10941285
doi:
Types de publication
Journal Article
Langues
eng
Pagination
771-786Informations de copyright
© 2024 The Authors. Published by American Chemical Society.
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.