Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator

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Abstract

This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC50 = 30 nM) in vitro, and reaches high brain levels in both rats and mice after oral administration.

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Acknowledgment

The authors thank Mr. Jude Alfred for technical assistance.

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