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Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system

Identification of metabotropic glutamate receptor antagonists using an automated high-throughput screening system

Analytical Biochemistry 313(2): 246-254

Antagonists to the human metabotropic glutamate receptor subtype 5a(mGluR5a) have been implicated as potential therapeutics for the treatment of a variety of nervous system disorders, including pain, anxiety, and Parkinson's disease. To discover novel antagonists to the mGluR5a, a functional assay measuring agonist-induced intracellular calcium release was developed. The assay was used for the high-throughput screening of a large collection of compounds in single wells using a fully automated robotic platform. Primary high-throughput screening hits were subjected to a combination of data analysis and counterscreening assays to identify several compounds with both efficacy and selectivity for the metabotropic glutamate receptor target.

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Accession: 010786722

Download citation: RISBibTeXText

PMID: 12605861

DOI: 10.1016/s0003-2697(02)00608-5

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