3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)
3-(2-Ethoxy-4-{4-[3-hydroxy-2-methyl-4-(3-methylbutanoyl)phenoxy]butoxy}phenyl)propanoic acid: a brain penetrant allosteric potentiator at the metabotropic glutamate receptor 2 (mGluR2)
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DOI：
10.1016/j.bmcl.2005.02.078
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发表时间：
2005-05-02
影响因子：
2.7
通讯作者：
Pinkerton, AB
中科院分区：
文献类型：
--
作者：
Cube, RV;Vernier, JM;Pinkerton, AB
我们鉴定并合成了一种脑穿透性丙酸作为代谢型谷氨酸受体2的变构增强剂。为了提高其效力、增强水平和脑穿透能力而进行的构效关系研究发现了8(EC50=1200 nM，77%增强，119%大鼠脑/血浆，20MPK ip，脑水平5700 nM)。©2005爱思唯尔有限公司。保留所有权利。
We have identified and synthesized a brain penetrant propanoic acid as an allosteric potentiator of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency, level of potentiation and brain penetration led to the discovery of 8 (EC50 = 1200 nM, 77% potentiation, 119% brain/plasma in rat, 20 mpk ip, brain level of 5700 nM). © 2005 Elsevier Ltd. All rights reserved.