期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 10, 页码 3467-3472出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.03.088
关键词
Muscarinic acetylcholine receptor 1; M-1; Allosteric; Agonist; Bitopic; ML071; VU0364572
资金
- NIH
- NIMH [1RO1MH082867-01, 5T32MH065215-09]
This Letter describes the continued optimization of the MLPCN probe molecule ML071. After introducing numerous cyclic constraints and novel substitutions throughout the parent structure, we produced a number of more highly potent agonists of the M-1 mACh receptor. While many novel agonists demonstrated a promising ability to increase soluble APP alpha release, further characterization indicated they may be functioning as bitopic agonists. These results and the implications of a bitopic mode of action are presented. (C) 2012 Elsevier Ltd. All rights reserved.
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