Synthesis and pharmacological evaluation of M4 muscarinic receptor positive allosteric modulators derived from VU10004

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Abstract

The M4 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 M4 PAMs derived from VU10004. These compounds investigate the pharmacological effects of target thieno[2,3-b]pyridines assembled from primary cycloalkanamines and cyclic secondary amines providing useful estimates of affinity (KB), cooperativity (a?), and direct agonist properties (B).
Original languageEnglish
Pages (from-to)838 - 844
Number of pages7
JournalACS Chemical Neuroscience
Volume6
Issue number6
DOIs
Publication statusPublished - 2015

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