Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M2R Affinity and Selectivity

URN to cite this document:: urn:nbn:de:bvb:355-epub-365386
DOI to cite this document:: 10.5283/epub.36538

She, Xueke ; Pegoli, Andrea ; Mayr, Judith ; Hübner, Harald ; Bernhardt, Günther

; Gmeiner, Peter ; Keller, Max

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Date of publication of this fulltext: 19 Jan 2018 11:46

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Abstract

In search for selective ligands for the muscarinic acetylcholine receptor (MR) subtype M-2, the dimeric ligand approach, that is combining two pharmacophores in one and the same molecule, was pursued. Different types (agonists, antagonists, orthosteric, and allosteric) of monomeric MR ligands were combined by various linkers with a dibenzodia-zepinone-type MR antagonist, affording five types of ...