Probing structural requirements of positive allosteric modulators of the M4 muscarinic receptor

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Abstract

The M, mAChR is implicated in several CNS disorders and possesses an allosteric binding site for which ligands modulating the affinity and/or efficacy of ACh may be exploited for selective receptor targeting. We report the synthesis of a focused library of putative M-4 PAMs derived from VU0152100 and VU10005. These compounds investigate the pharmacological effects of previously identified methoxy and fluoro substituents, providing useful estimates of affinity (K-B), cooperativity (alpha beta), and direct agonist properties (tau(B)).
Original languageEnglish
Pages (from-to)8196 - 8200
Number of pages5
JournalJournal of Medicinal Chemistry
Volume56
Issue number20
DOIs
Publication statusPublished - 2013

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