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Peer-reviewed veterinary case report

Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 3: Identification and biological activity of indanone containing mGlu2 receptor potentiators.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2005
Authors:
Pinkerton, Anthony B et al.
Affiliation:
Merck Research Laboratories · United States

Abstract

We have identified and synthesized a series of phenyl-tetrazolyl and 4-thiopyridyl indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure activity relationship studies directed toward improving the potency and level of potentiation, as well as PK properties, led to the discovery of 28 (EC50=186 nM), which displayed activity in a rodent model for schizophrenia.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/15745798/