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.

Gespeichert in:
Bibliographische Detailangaben
Hauptverfasser: 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.
Format: Artigo
Sprache:Inglês
Veröffentlicht: 2011
Schlagworte:
Article
Online Zugang: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
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!

Ähnliche Einträge