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)
- Carson W. Reed (4585258)
- Samantha E. Yohn (579063)
- Jordan P. Washecheck (6237290)
- Hanna F. Roenfanz (4585252)
- Marc C. Quitalig (6237293)
- Vincent B. Luscombe (3595577)
- Matthew T. Jenkins (6237296)
- Alice L. Rodriguez (1270236)
- Darren W. Engers (655505)
- Anna L. Blobaum (1284048)
- P. Jeffrey Conn (1270239)
- Colleen M. Niswender (353419)
- Craig W. Lindsley (203380)
Publication date
January 2019
DOI Publisher
American Chemical Society (ACS)Abstract
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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