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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 and Read, Roger W. (2015) M2 subtype preferring dibenzodiazepinone-type muscarinic receptor ligands: effect of chemical homo-dimerization on orthosteric (and allosteric?) binding. Bioorganic & Medicinal Chemistry 23 (14), pp. 3970-3990.

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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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Item type:Article
Date:2015
Additional Information (public):Supplementary material available. Cf. http://www.sciencedirect.com/science/article/pii/S0968089615000188
Institutions:Chemistry and Pharmacy > Institute of Pharmacy > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer)
Projects:GRK 1910, Graduiertenkolleg "Medicinal Chemistry of Selective GPCR Ligands"
Identification Number:
ValueType
10.1016/j.bmc.2015.01.015DOI
25650309PubMed ID
Related URLs:
URLURL Type
http://www.sciencedirect.com/science/article/pii/S0968089615000188Publisher
Keywords:Muscarinic acetylcholine receptors; dibenzodiazepinones; antagonists; dimeric ligands; allosteric binding; AF-DX 384
Dewey Decimal Classification:500 Science > 540 Chemistry & allied sciences
600 Technology > 615 Pharmacy
Status:Published
Refereed:Yes, this version has been refereed
Created at the University of Regensburg:Partially
Item ID:30900
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