Article
A novel class of succinimide-derived negative allosteric modulators of metabotropic glutamate receptor subtype 1 provides insight into a disconnect in activity between the rat and human receptors.
ACS chemical neuroscience - 16 Jul 2014
Cho Hyekyung P, Engers Darren W, Venable Daryl F, Niswender Colleen M, Lindsley Craig W, Conn P Jeffrey, Emmitte Kyle A, Rodriguez Alice L
Abstract excerpt
Recent progress in the discovery of mGlu₁ allosteric modulators has suggested the modulation of mGlu₁ could offer possible treatment for a number of central nervous system disorders; however, the available chemotypes are inadequate to fully investigate the therapeutic potential of mGlu₁ modulation. To address this issue, we used a fluorescence-based high-throughput screening assay to screen an allosteric...
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