Discovery of VU2957 (Valiglurax): An mGlu(4) Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson’s Disease

[Image: see text] Herein, we report the discovery of a novel potent, selective, CNS penetrant, and orally bioavailable mGlu(4) PAM, VU0652957 (VU2957, Valiglurax). VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties across species. To advance toward the clinic, a spr...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:ACS Med Chem Lett
Hauptverfasser: Panarese, Joseph D., Engers, Darren W., Wu, Yong-Jin, Bronson, Joanne J., Macor, John E., Chun, Aspen, Rodriguez, Alice L., Felts, Andrew S., Engers, Julie L., Loch, Matthew T., Emmitte, Kyle A., Castelhano, Arlindo L., Kates, Michael J., Nader, Michael A., Jones, Carrie K., Blobaum, Anna L., Conn, P. Jeffrey, Niswender, Colleen M., Hopkins, Corey R., Lindsley, Craig W.
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2018
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6421540/
https://ncbi.nlm.nih.gov/pubmed/30891122
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.8b00426
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!

Ähnliche Einträge