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M2 subtype preferring dibenzodiazepinone-type muscarinic receptor ligands: effect of chemical homo-dimerization on orthosteric (and allosteric?) binding

Keller, Max ; Tränkle, Christian ; She, Xueke ; Pegoli, Andrea ; Bernhardt, Günther ; Buschauer, Armin ; Read, Roger W.



Abstract

A series of new dibenzodiazepinone-type muscarinic receptor ligands, including two homo-dimeric compounds, was prepared. Sixteen representative compounds were characterized in equilibrium binding studies with [3H]N-methylscopolamine ([3H]NMS) at the muscarinic receptor subtype M2, and seven selected compounds were additionally investigated at M1, M3, M4 and M5 with respect to receptor subtype ...

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