Discovery of VU0431316: A negative allosteric modulator of mGlu(5) with activity in a mouse model of anxiety

Development of SAR in an aryl ether series of mGlu(5) NAMs leading to the identification of pyrazine analog VU0431316 is described in this Letter. VU0431316 is a potent and selective non-competitive antagonist of mGlu(5) that binds at a known allosteric binding site. VU0431316 demonstrates an attrac...

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Bibliografische gegevens
Hoofdauteurs: Bates, Brittney S., Rodriguez, Alice L., Felts, Andrew S., Morrison, Ryan D., Venable, Daryl F., Blobaum, Anna L., Byers, Frank W., Lawson, Kera P., Daniels, J. Scott, Niswender, Colleen M., Jones, Carrie K., Conn, P. Jeffrey, Lindsley, Craig W., Emmitte, Kyle A.
Formaat: Artigo
Taal:Inglês
Gepubliceerd in: 2014
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Article
Online toegang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4090943/
https://ncbi.nlm.nih.gov/pubmed/24969015
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2014.06.003
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