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Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 May 15; Vol. 22 (10), pp. 3467-72. Date of Electronic Publication: 2012 Mar 29. - Publication Year :
- 2012
-
Abstract
- 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 APPĪ± release, further characterization indicated they may be functioning as bitopic agonists. These results and the implications of a bitopic mode of action are presented.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Humans
Molecular Probes
Receptors, Muscarinic drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22507963
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.03.088