Title of article
Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
6
From page
885
To page
890
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799077
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