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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)
dataset
posted on 2019-01-04, 00:00 authored by 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. LindsleyHerein, 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.
