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)
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数据链接:
https://figshare.com/articles/dataset/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_/7597598数据链接链接失效反馈
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资源简介:
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.
创建时间:
2019-01-16



