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 language | English |
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Pages (from-to) | 8196 - 8200 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 56 |
Issue number | 20 |
DOIs | |
Publication status | Published - 2013 |