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Discovery of an Orally Bioavailable and Central Nervous System (CNS) Penetrant mGlu(7) 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)

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 preclin...

詳細記述

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書誌詳細
出版年:J Med Chem
主要な著者: Reed, Carson W., Yohn, Samantha E., Washecheck, Jordan P., Roenfanz, Hanna F., Quitalig, Marc C., Luscombe, Vincent B., Jenkins, Matthew T., Rodriguez, Alice L., Engers, Darren W., Blobaum, Anna L., Conn, P. Jeffrey, Niswender, Colleen M., Lindsley, Craig W.
フォーマット: Artigo
言語:Inglês
出版事項: 2019
主題:
オンライン・アクセス:https://ncbi.nlm.nih.gov/pmc/articles/PMC6501583/
https://ncbi.nlm.nih.gov/pubmed/30608678
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01810
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