Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 21, Issue 21, Pages 6451-6455Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.08.084
Keywords
Muscarinic acetylcholine receptor 1; mAChR1 (M-1); ML071; Allosteric agonist
Categories
Funding
- NIH
- NIMH [1RO1MH082867-01]
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Herein we report the discovery and SAR of a novel series of M-1 agonists based on the MLPCN probe, ML071. From this, VU0364572 emerged as a potent, orally bioavailable and CNS penetrant M-1 agonist with high selectivity, clean ancillary pharmacology and enantiospecific activity. (C) 2011 Elsevier Ltd. All rights reserved.
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