1.
ACS Chem Neurosci
; 6(6): 838-44, 2015 Jun 17.
Artigo
em Inglês
| MEDLINE
| ID: mdl-25857219
RESUMO
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 (αß), and direct agonist properties (τB).