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Discovery of a potent and brain penetrant mGluR5 positive allosteric modulator |
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| Authors: | Andreas Ritzén Rikke Sindet Morten Hentzer Nannette Svendsen Robbin M. Brodbeck Christoffer Bundgaard |
| Affiliation: | 1. Medicinal Chemistry Research DK, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark;2. Molecular Pharmacology, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark;3. Drug Discovery Biology, Lundbeck Research USA, Inc., 215 College Road, Paramus, NJ 07652-1431, USA;4. Discovery ADME, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark |
| 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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