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Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M2 Receptor

She, Xueke ; Pegoli, Andrea ; Gruber, Corinna G. ; Wifling, David ; Carpenter, Jessica ; Hübner, Harald ; Chen, Mengya ; Wan, Jianfei ; Bernhardt, Günther ; Gmeiner, Peter ; Holliday, Nicholas D. ; Keller, Max


Fluorescently labeled dibenzodiazepinone-type muscarinic acetylcholine receptor (MR) antagonists, including dimeric ligands, were prepared using red-emitting cyanine dyes. Probes containing a fluorophore with negative charge showed high M2R affinities (pK(i) (radioligand competition binding): 9.10-9.59). Binding studies at M-1 and M-3-M-5 receptors indicated a M2R preference. Flow cytometric and ...


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