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

Carson W Reed,Samantha E Yohn,Jordan P Washecheck,Hanna F Roenfanz,Marc C Quitalig,Vincent B Luscombe,Matthew T Jenkins,Alice L Rodriguez,Darren W Engers,Anna L Blobaum,P Jeffrey Conn,Colleen M Niswender,Craig W Lindsley

JOURNAL OF MEDICINAL CHEMISTRY（2019）

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摘要

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

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关键词

vivo tool compound,penetrant mglu<sub>7</sub>,negative allosteric modulator,nervous system

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