Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 23, Issue 6, Pages 1860-1864Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.01.017
Keywords
Muscarinic acetylcholine receptor 1; M-1; Spirocyclic; Positive allosteric modulator (PAM); ML137; VU0413162
Categories
Funding
- NIH [U54MH084659]
- NIMH [1RO1MH082867]
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This Letter describes the further optimization of an MLPCN probe molecule (ML137) through the introduction of 5- and 6-membered spirocycles in place of the isatin ketone. Interestingly divergent structure-activity relationships, when compared to earlier M-1 PAMs, are presented. These novel spirocycles possess improved efficacy relative to ML137, while also maintaining high selectivity for the human and rat muscarinic M-1 receptor subtype. (C) 2013 Elsevier Ltd. All rights reserved.
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