Author/Authors :
L. Michelle Lewis، نويسنده , , Douglas Sheffler، نويسنده , , Richard Williams، نويسنده , , Thomas M. Bridges، نويسنده , , J. Phillip Kennedy، نويسنده , , J.T. Brogan، نويسنده , , Matthew J. Mulder، نويسنده , , Lyndsey Williams، نويسنده , , Natalia T. Nalywajko، نويسنده , , Colleen M. Niswender، نويسنده , , Charles D. Weaver، نويسنده , , P. Jeffrey Conn، نويسنده , , Craig W. Lindsley، نويسنده ,
Abstract :
This Letter describes the synthesis and SAR, developed through an iterative analogue library approach, of a novel series of selective M1 mAChR antagonists for the potential treatment of Parkinson’s disease, dystonia and other movement disorders. Compounds in this series possess M1 antagonist IC50s in the 441 nM–19 μM range with 8- to >340-fold functional selectivity versus rM2–rM5.
Keywords :
M1 , Muscarinic acetylcholine receptors , Antagonist , Dystonia , G protein-coupled receptors
