Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 2, Pages 558-562Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.11.089
Keywords
M5; Muscarinic receptor; Allosteric; Positive allosteric modualtor; PAM
Categories
Funding
- NIMH [1RO1 MH082867]
- NIH
- MLPCN [1U54 MH084659]
- Alzheimer's Association [IIRG- 0757131]
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This 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 @ 30 mu M), and an important tool compound to study the role of M-5 in the CNS. (C) 2009 Elsevier Ltd. All rights reserved.
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