Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu(4)) antagonist: Unexpected ‘molecular switch’ from a closely related mGlu(4) positive allosteric modulator

Herein we report the discovery and SAR of a novel antagonist of metabotropic glutamate receptor 4 (mGlu(4)). The antagonist was discovered via a molecular switch from a closely related mGlu(4) positive allosteric modulator (PAM). This antagonist (VU0448383) displays an IC(50) value of 8.2 ± 0.4 μM a...

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Autori principali: Utley, Thomas, Haddenham, Dustin, Salovich, James M., Zamorano, Rocio, Vinson, Paige N., Lindsley, Craig W., Hopkins, Corey R., Niswender, Colleen M.
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2011
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Article
Accesso online:https://ncbi.nlm.nih.gov/pmc/articles/PMC3319082/
https://ncbi.nlm.nih.gov/pubmed/22030026
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2011.09.131
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