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Article 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 APPα release, further characterization indicated they may be functioning as bitopic agonists. These results and the implications of a bitopic mode of action are presented.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3348459 | PMC |
| http://dx.doi.org/10.1016/j.bmcl.2012.03.088 | DOI Listing |
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