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Issue 8, 2010
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Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders

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Abstract

Muscarinic acetylcholine receptors (mAChRs) represent exciting therapeutic targets for the treatment of multiple CNS disorders. The high degree of conservation of amino acids comprising the orthosteric acetylcholine (ACh) binding site between individual mAChR subtypes has hindered the development of subtype-selective compounds that bind to this site. As a result, many academic and industry researchers are now focusing on developing allosteric activators of mAChRs including both positive allosteric modulators (PAMs) and allosteric agonists. In the past 10 years major advances have been achieved in the discovery of allosteric ligands that possess much greater selectivity for individual mAChR subtypes when compared to previously developed orthosteric agents. These novel allosteric modulators of mAChRs may provide therapeutic potential for treatment of a number of CNS disorders such as Alzheimer’s disease and schizophrenia.

Graphical abstract: Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders

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Submitted
15 Feb 2010
Accepted
19 May 2010
First published
25 Jun 2010

Mol. BioSyst., 2010,6, 1345-1354
Article type
Review Article

Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders

G. J. Digby, J. K. Shirey and P. J. Conn, Mol. BioSyst., 2010, 6, 1345
DOI: 10.1039/C002938F

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