Development of a Highly Selective, Orally Bioavailable and CNS Penetrant M(1) Agonist Derived from the MLPCN Probe ML071

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.

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Detalhes bibliográficos
Main Authors: Lebois, Evan P., Digby, Gregory J., Sheffler, Douglas J., Melancon, Bruce J., Tarr, James C., Cho, Hyekyung P., Miller, Nicoel R., Morrison, Ryan, Bridges, Thomas M., Xiang, Zixiu, Daniels, J. Scott, Wood, Michael R., Conn, P. Jeffrey, Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2011
Assuntos:
Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3190051/
https://ncbi.nlm.nih.gov/pubmed/21930376
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2011.08.084
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