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...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2018
Acesso em linha: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
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