Discovery of VU6027459: A First-in-Class Selective and CNS Penetrant mGlu(7) Positive Allosteric Modulator Tool Compound

[Image: see text] Herein, we report the discovery of the first selective and CNS penetrant mGlu(7) PAM (VU6027459) derived from a “molecular switch” within a selective mGlu(7) NAM chemotype. VU6027459 displayed CNS penetration in both mice (K(p) = 2.74) and rats (K(p)= 4.78), it was orally bioavaila...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Reed, Carson W., Kalbfleisch, Jacob J., Wong, Madison J., Washecheck, Jordan P., Hunter, Ashton, Rodriguez, Alice L., Blobaum, Anna L., Conn, P. Jeffrey, Niswender, Colleen M., Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2020
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC7488291/
https://ncbi.nlm.nih.gov/pubmed/32944146
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00432
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