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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...
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| 出版年: | J Med Chem |
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| 主要な著者: | , , , , , , , , , , , , |
| フォーマット: | Artigo |
| 言語: | Inglês |
| 出版事項: |
2019
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| 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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