Bicyclic Metabotropic Glutamate Receptor Ligands
Compounds of the invention demonstrate significantly higher potency for mGluRs than (1S, 3R)-ACPD.
Glutamate receptors play a role in numerous neurological,neurodegenerative, psychiatric and psychological disease states. Newderivatives of the glutamate agonist, (1S, 3R)-1-aminocyclopentane-1,3-dicarboxylic acid [(1S, 3R)-ACPD],have been synthesized and screened for potency and biological activity.Biological data supports the activity of these compounds for a varietyof mGluRs. In-vitro studies reveal that a specific novel bicycliccompound, ABHxD-I, is between 6 to 34-fold more potent in EC50 assays for mGluRs than (1S, 3R)-ACPD.These compounds demonstrate potential as therapeutic agents inpharmaceutical compositions and can be used in research to probe mGluRfunction.
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