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Conjugation of Short Peptides to Dibenzodiazepinone-Type
Muscarinic Acetylcholine Receptor Ligands Determines M2R
Selectivity

Pegoli, Andrea ; Wifling, David ; Gruber, Corinna G. ; Xueke, She ; Hübner, Harald ; Bernhardt, Günther ; Gmeiner, Peter ; Keller, Max



Abstract

Muscarinic acetylcholine receptors (MRs), comprising five subtypes (M1R-M5R) in humans, exhibit a high degree of structural similarity. Therefore, subtype selective MR agonists and antagonists are lacking. We present an approach to highly M2R-selective MR antagonists based on the conjugation of di- or tripeptides to M2R-preferring dibenzodiazepinone-type MR antagonists. M2R selectivity was ...

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