Development of a novel, CNS-penetrant, metabotropic glutamate receptor 3 (mGlu(3)) NAM probe (ML289) derived from a closely related mGlu(5) PAM

Herein we report the discovery and SAR of a novel metabotropic glutamate receptor 3 (mGlu3) NAM probe (ML289) with 15-fold selectivity versus mGlu2. The mGlu3 NAM was discovered via a ‘molecular switch’ from a closely related, potent mGlu5 positive allosteric modulator (PAM), VU0092273. This NAM (VU...

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Main Authors: Sheffler, Douglas J., Wenthur, Cody J., Bruner, Joshua A., Carrington, Sheridan J.S., Vinson, Paige N., Gogi, Kiran K., Blobaum, Anna L., Morrison, Ryan D., Vamos, Mitchell, Cosford, Nicholas D. P., Stauffer, Shaun R., Daniels, J. Scott, Niswender, Colleen M., Conn, P. Jeffrey, Lindsley, Craig W.
Formato: Artigo
Idioma:Inglês
Publicado em: 2012
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3365510/
https://ncbi.nlm.nih.gov/pubmed/22607673
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2012.04.112
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