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Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu7 Negative Allosteric Modulator (NAM) in Vivo Tool Compound: N-(2-(1H-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
1 ,
Colleen M. Niswender
1 ,
Craig W. Lindsley
January 17 2019
January 17 2019
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Abstract
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) 2.5× above the in vitro IC 50 at minimum effective
doses (MEDs) of 3 mg/kg in preclinical anxiety models.