| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1372131 | Bioorganic & Medicinal Chemistry Letters | 2011 | 5 Pages |
Abstract
Herein we report the discovery and SAR of a novel antagonist of metabotropic glutamate receptor 4 (mGlu4). The antagonist was discovered via a molecular switch from a closely related mGlu4 positive allosteric modulator (PAM). This antagonist (VU0448383) displays an IC50 value of 8.2 ± 0.4 μM and inhibits an EC80 glutamate response by 63.1 ± 6.6%.
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Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Thomas Utley, Dustin Haddenham, James M. Salovich, Rocio Zamorano, Paige N. Vinson, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender,