Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors.

Marino MJ, Conn PJ
Curr Opin Pharmacol. 2006 6 (1): 98-102

PMID: 16368268 · DOI:10.1016/j.coph.2005.09.006

Metabotropic glutamate receptors (mGluRs) have been proposed as novel targets for the treatment of a variety of disorders. Recently, highly selective allosteric modulators of the mGluRs have been developed by several groups. These allosteric compounds provide an unprecedented degree of selectivity for individual mGluRs, allowing for more detailed functional studies on the roles of these receptors. Furthermore, the allosteric approach avoids many of the hurdles associated with the development of direct agonists as drugs, and provides a clear path forward for clinical proof-of-concept studies. Currently, both positive allosteric modulators of mGluR2 and negative allosteric modulators of mGluR5 hold promise as novel anxiolytics, and positive allosteric modulators of mGluR4 appear to be an exciting new target for the treatment of Parkinson's disease.

MeSH Terms (14)

Animals Anxiety Benzopyrans Clinical Trials as Topic Drug Evaluation, Preclinical Excitatory Amino Acid Agonists Excitatory Amino Acid Antagonists Humans Imidazoles Parkinson Disease Pyridines Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate Sulfonamides

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