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Synthesis and SAR of a novel metabotropic glutamate receptor 4 (mGlu4) antagonist: unexpected 'molecular switch' from a closely related mGlu4 positive allosteric modulator |
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| Authors: | Utley Thomas Haddenham Dustin Salovich James M Zamorano Rocio Vinson Paige N Lindsley Craig W Hopkins Corey R Niswender Colleen M |
| Institution: | Department of Pharmacology, Vanderbilt University Medical Center, Nashville, TN 37232, USA. |
| Abstract: | 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 and inhibits an EC(80) glutamate response by 63.1±6.6%. |
| Keywords: | Metabotropic glutamate receptor 4 mGlu4 Molecular switch Antagonist |
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