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Bioorg. Med. Chem. Lett. · Jan 2010
Chemical lead optimization of a pan G(q) mAChR M(1), M(3), M(5) positive allosteric modulator (PAM) lead. Part I: Development of the first highly selective M(5) PAM.
- Thomas M Bridges, J Phillip Kennedy, Hyekyung P Cho, Micah L Breininger, Patrick R Gentry, Corey R Hopkins, P Jeffrey Conn, and Craig W Lindsley.
- Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA.
- Bioorg. Med. Chem. Lett. 2010 Jan 15; 20 (2): 558-62.
AbstractThis Letter describes a chemical lead optimization campaign directed at VU0238429, the first M(5)-preferring positive allosteric modulator (PAM), discovered through analog work around VU0119498, a pan G(q) mAChR M(1), M(3), M(5) PAM. An iterative library synthesis approach delivered the first selective M(5) PAM (no activity at M(1)-M(4) @ 30microM), and an important tool compound to study the role of M(5) in the CNS.Copyright 2009 Elsevier Ltd. All rights reserved.
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