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Novel BQCA‐ and TBPB‐Derived M 1 Receptor Hybrid Ligands: Orthosteric Carbachol Differentially Regulates Partial Agonism

Schramm, Simon ; Agnetta, Luca ; Bermudez, Marcel ; Gerwe, Hubert ; Irmen, Matthias ; Holze, Janine ; Littmann, Timo ; Wolber, Gerhard ; Tränkle, Christian ; Decker, Michael


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, ...


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