VU6012962(VU6012962) - 药物靶点：mGluR7_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

mGluR7

作用方式

调节剂

作用机制

mGluR7调节剂(代谢型谷氨酸受体-7调节剂)

治疗领域

神经系统疾病

在研适应症-

非在研适应症

中枢神经系统疾病

原研机构

Vanderbilt University

在研机构-

非在研机构

Vanderbilt University

权益机构-

最高研发阶段无进展临床前

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构/序列

分子式C21H19F3N4O4

InChIKeyIQNLJJLZIVCGFI-UHFFFAOYSA-N

CAS号2313526-86-0

关联

100 项与 VU6012962 相关的临床结果

登录后查看更多信息

100 项与 VU6012962 相关的转化医学

登录后查看更多信息

100 项与 VU6012962 相关的专利（医药）

登录后查看更多信息

2

项与 VU6012962 相关的文献（医药）

2022-10-01·Bioorganic & Medicinal Chemistry Letters

Development and profiling of mGlu7 NAMs with a range of saturable inhibition of agonist responses in vitro

Article

作者: Blobaum, Anna L ; Jenkins, Matthew T ; Lindsley, Craig W ; Reed, Carson W ; Kalbfleisch, Jacob J ; Niswender, Colleen M ; Seto, Mabel ; Rodriguez, Alice L ; Chang, Sichen

We describe here a series of metabotropic glutamate receptor 7 (mGlu₇) negative allosteric modulators (NAMs) with a saturable range of activity in inhibiting responses to an orthosteric agonist in two distinct in vitro pharmacological assays. The range of inhibition among compounds in this scaffold provides highly structurally related ligands with differential degrees of receptor blockade that can be used to understand inhibitory efficacy profiles in native tissue or in vivo.

2019-02-14·Journal of Medicinal Chemistry1区 · 医学

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)

1区 · 医学

Article

作者: Luscombe, Vincent B. ; Reed, Carson W. ; Niswender, Colleen M. ; Blobaum, Anna L. ; Engers, Darren W. ; Jenkins, Matthew T. ; Rodriguez, Alice L. ; Conn, P. Jeffrey ; Yohn, Samantha E. ; Quitalig, Marc C. ; Washecheck, Jordan P. ; Roenfanz, Hanna F. ; Lindsley, Craig W.

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.

100 项与 VU6012962 相关的药物交易

登录后查看更多信息