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Issue 7, 2012
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M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease

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Abstract

In this review the various chemical structures of allosteric agonists and modulators of the muscarinic acetylcholine receptor subtype 1 (mAChR1 or M1) 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. M1 bitopic ligands and hybrid molecules are also considered. All these differently designed M1 allosteric modulators open exciting new paths in medicinal chemistry with most promising therapeutic opportunities to fight AD.

Graphical abstract: M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease

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Publication details

The article was received on 31 Jan 2012, accepted on 03 Mar 2012 and first published on 12 Mar 2012


Article type: Review Article
DOI: 10.1039/C2MD20025B
Citation: Med. Chem. Commun., 2012,3, 752-762
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    M1 muscarinic cetylcholine receptor allosteric modulators as potential therapeutic opportunities for treating Alzheimer's disease

    M. Decker and U. Holzgrabe, Med. Chem. Commun., 2012, 3, 752
    DOI: 10.1039/C2MD20025B

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