She, Xueke, Pegoli, Andrea, Mayr, Judith, Hübner, Harald, Bernhardt, Günther 
, Gmeiner, Peter and Keller, Max
(2017)
Heterodimerization of Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Leads to Increased M2R Affinity and Selectivity.
ACS Omega 2 (10), pp. 6741-6754.
| License: Creative Commons Attribution 4.0 PDF - Submitted Version Download (2MB) |
Other URL: http://doi.org/10.1021/acsomega.7b01085, http://pubs.acs.org/doi/full/10.1021/acsomega.7b01085
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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 ...
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| Item type: | Article | ||||
|---|---|---|---|---|---|
| Date: | 16 October 2017 | ||||
| Institutions: | Chemistry and Pharmacy > Institute of Pharmacy | ||||
| Projects: | Open Access Publizieren (DFG) | ||||
| Identification Number: |
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| Keywords: | PROTEIN-COUPLED RECEPTORS; ALLOSTERIC BINDING-SITES; BITOPIC LIGANDS; RESIDENCE TIME; HIGHLY POTENT; M-2 RECEPTOR; ANTAGONIST; AGONISTS; MODULATORS; DESIGN; | ||||
| Dewey Decimal Classification: | 600 Technology > 615 Pharmacy | ||||
| Status: | Published | ||||
| Refereed: | Yes, this version has been refereed | ||||
| Created at the University of Regensburg: | Yes | ||||
| Item ID: | 36538 |
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