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Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu<sub>7</sub> Negative Allosteric Modulator (NAM) in Vivo Tool Compound: <i>N</i>‑(2-(1<i>H</i>‑1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)-4-(cyclopropylmethoxy)-3-methoxybenzamide (VU6012962)

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NIAID Data Ecosystem2026-03-10 收录
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Herein, we report the discovery of a new, orally bioavailable and CNS-penetrant metabotropic glutamate receptor 7 (mGlu7) negative allosteric modulator (NAM) that achieves exposure in cerebral spinal fluid (CSF) 2.5× above the in vitro IC50 at minimum effective doses (MEDs) of 3 mg/kg in preclinical anxiety models.

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2019-01-16
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