From 2-Triethylammonium Ethyl Ether of 4-Stilbenol (MG624) to Selective Small-Molecule Antagonists of Human α9α10 Nicotinic Receptor by Modifications at the Ammonium Ethyl Residue.
Journal
Journal of medicinal chemistry
ISSN: 1520-4804
Titre abrégé: J Med Chem
Pays: United States
ID NLM: 9716531
Informations de publication
Date de publication:
28 07 2022
28 07 2022
Historique:
pubmed:
15
7
2022
medline:
30
7
2022
entrez:
14
7
2022
Statut:
ppublish
Résumé
Nicotinic acetylcholine receptors containing α9 subunits (α9*-nAChRs) are potential druggable targets arousing great interest for pain treatment alternative to opioids. Nonpeptidic small molecules selectively acting as α9*-nAChRs antagonists still remain an unattained goal. Here, through modifications of the cationic head and the ethylene linker, we have converted the 2-triethylammonium ethyl ether of 4-stilbenol (MG624), a well-known α7- and α9*-nAChRs antagonist, into some selective antagonists of human α9*-nAChR. Among these, the compound with cyclohexyldimethylammonium head (
Identifiants
pubmed: 35834819
doi: 10.1021/acs.jmedchem.2c00746
pmc: PMC9339509
mid: NIHMS1824089
doi:
Substances chimiques
Ammonium Compounds
0
Nicotinic Antagonists
0
Quaternary Ammonium Compounds
0
Receptors, Nicotinic
0
Stilbenes
0
Ether
0F5N573A2Y
triethyl-(beta-4-stilbenoxyethyl)ammonium
2551-76-0
4-hydroxystilbene
3839-46-1
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Langues
eng
Sous-ensembles de citation
IM
Pagination
10079-10097Subventions
Organisme : NIDA NIH HHS
ID : R01 DA042749
Pays : United States
Organisme : NIDA NIH HHS
ID : R01 DA043567
Pays : United States
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