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Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M2 Muscarinic Acetylcholine Receptor

Pegoli, Andrea , She, Xueke, Wifling, David , Hübner, Harald, Bernhardt, Günther, Gmeiner, Peter and Keller, Max (2017) Radiolabeled Dibenzodiazepinone-Type Antagonists Give Evidence of Dualsteric Binding at the M2 Muscarinic Acetylcholine Receptor. Journal of Medicinal Chemistry 60 (8), pp. 3314-3334.

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Other URL: http://doi.org/10.1021/acs.jmedchem.6b01892


Abstract

The dualsteric ligand approach, aiming at ligands with improved subtype selectivity, has been increas-X ingly applied to muscarinic receptors (MRs). In this article, we present the synthesis and characterization of a M2R subtype preferring radiolabeled dibenzodiazepinone-type antagonist ([H-3]UNSW-MK259, [H-3]19) and its homodimeric analogue [H-3]UR-AP060 ([H-3]33). Saturation binding studies at ...

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Item type:Article
Date:2017
Institutions:Chemistry and Pharmacy > Institute of Pharmacy
Identification Number:
ValueType
10.1021/acs.jmedchem.6b01892DOI
Keywords:MOLECULAR-DYNAMICS SIMULATIONS; GENERAL FORCE-FIELD; PROTEIN-COUPLED RECEPTORS; ALLOSTERIC MODULATORS; ALZHEIMERS-DISEASE; LIGAND-BINDING; NEUROPEPTIDE-Y; RESIDENCE TIME; CNS DISORDERS; CHARMM;
Dewey Decimal Classification:600 Technology > 615 Pharmacy
500 Science > 540 Chemistry & allied sciences
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Yes
Item ID:36110
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