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  • Title: Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator.
    Author: Ritzén A, Sindet R, Hentzer M, Svendsen N, Brodbeck RM, Bundgaard C.
    Journal: Bioorg Med Chem Lett; 2009 Jun 15; 19(12):3275-8. PubMed ID: 19443216.
    Abstract:
    This Letter describes the discovery of a novel series of mGluR5 positive allosteric modulators (PAMs). The lead compound, 11c, exhibits excellent potency (EC(50)=30 nM) in vitro, and reaches high brain levels in both rats and mice after oral administration.
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