M-1 muscarinic acetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease

Decker, Michael and Holzgrabe, Ulrike (2012) M-1 muscarinic acetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease. MEDCHEMCOMM, 3 (7). pp. 752-762. ISSN 2040-2503

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Abstract

In this review the various chemical structures of allosteric agonists and modulators of the muscarinic acetylcholine receptor subtype 1 (mAChR(1) or M-1) and their relevance for possible treatment of Alzheimer's disease (AD) are discussed. Furthermore, their design principles, common structural properties and their unique features with regard to structure-activity relationships (SARs), such as 'molecular switches' and 'steep/flat' SARs, are highlighted. M-1 bitopic ligands and hybrid molecules are also considered. All these differently designed M-1 allosteric modulators open exciting new paths in medicinal chemistry with most promising therapeutic opportunities to fight AD.

Item Type: Article
Uncontrolled Keywords: FUNCTIONAL SELECTIVITY; BIVALENT LIGANDS; AGONISTS AC-42; CNS PENETRANT; MUTANT MICE; DISCOVERY; ACTIVATION; DISORDERS; MECHANISM; DISTINCT;
Subjects: 600 Technology > 615 Pharmacy
Divisions: Chemistry and Pharmacy > Institute of Pharmacy
Depositing User: Petra Gürster
Date Deposited: 18 May 2020 05:56
Last Modified: 18 May 2020 05:56
URI: https://pred.uni-regensburg.de/id/eprint/18524

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