Novel BQCA- and TBPB-Derived M
GPCRs
allostery
dualsteric ligands
muscarinic receptors
partial agonists
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
17 07 2019
17 07 2019
Historique:
received:
09
05
2019
revised:
05
06
2019
pubmed:
6
6
2019
medline:
7
7
2020
entrez:
6
6
2019
Statut:
ppublish
Résumé
Recently, investigations of the complex mechanisms of allostery have led to a deeper understanding of G protein-coupled receptor (GPCR) activation and signaling processes. In this context, muscarinic acetylcholine receptors (mAChRs) are highly relevant due to their exemplary role in the study of allosteric modulation. In this work, we compare and discuss two sets of putatively dualsteric ligands, which were designed to connect carbachol to different types of allosteric ligands. We chose derivatives of TBPB [1-(1'-(2-tolyl)-1,4'-bipiperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one] as M
Identifiants
pubmed: 31166078
doi: 10.1002/cmdc.201900283
doi:
Substances chimiques
1-(1'-(2-methylbenzyl)-1,4'-bipiperidin-4-yl)-1H-benzo(d)imidazol-2-(3H)-one
0
1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
0
Benzimidazoles
0
Ligands
0
Muscarinic Agonists
0
Piperidines
0
Quinolines
0
Receptor, Muscarinic M1
0
Carbachol
8Y164V895Y
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
1349-1358Informations de copyright
© 2019 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.