Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596015 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
This Letter describes the continued optimization of an MLPCN probe molecule (ML137) with a focused effort on the replacement/modification of the isatin moiety present in this highly selective M1 PAM. A diverse range of structures were validated as viable replacements for the isatin, many of which engendered sizeable improvements in their ability to enhance the potency and efficacy of acetylcholine when compared to ML137. Muscarinic receptor subtype selectivity for the M1 receptor was also maintained.
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Authors
Bruce J. Melancon, Michael S. Poslusney, Patrick R. Gentry, James C. Tarr, Douglas J. Sheffler, Margrith E. Mattmann, Thomas M. Bridges, Thomas J. Utley, J. Scott Daniels, Colleen M. Niswender, P. Jeffrey Conn, Craig W. Lindsley, Michael R. Wood,