Discovery of “Molecular Switches” within a Series of mGlu(5) Allosteric Ligands Driven by a “Magic Methyl” Effect Affording Both PAMs and NAMs with In Vivo Activity, Derived from an M(1) PAM Chemotype

[Image: see text] In the course of optimizing an M(1) PAM chemotype, introduction of an ether moiety unexpectedly abolished M(1) PAM activity while engendering a “molecular switch” to afford a weak, pure mGlu(5) PAM. Further optimization was able to deliver a potent (mGlu(5) EC(50) = 520 nM, 63% Glu...

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Detalles Bibliográficos
Autores principales: Barbaro, Lisa, Rodriguez, Alice L., Blevins, Ashlyn N., Dickerson, Jonathan W., Billard, Natasha, Boutaud, Olivier, Rook, Jerri L., Niswender, Colleen M., Conn, P.Jeffrey, Engers, Darren W., Lindsley, Craig W.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2021
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10114714/
https://www.ncbi.nlm.nih.gov/pubmed/37101980
http://dx.doi.org/10.1021/acsbiomedchemau.1c00024

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