Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor
Biphenyl-indanones: Allosteric potentiators of the metabotropic glutamate subtype 2 receptor
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DOI：
10.1016/j.bmcl.2005.06.062
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发表时间：
2005-10-01
影响因子：
2.7
通讯作者：
Kamenecka, TM
中科院分区：
文献类型：
--
作者：
Bonnefous, C;Vernier, JM;Kamenecka, TM
我们已经鉴定并合成了一系列的联苯羧酸吲哚酮，作为代谢性谷氨酸受体2的变构增强剂。通过结构-活性关系研究，我们发现了5和23 （EC50分别为111 nM和5 nM）。(c) 2005 Elsevier Ltd版权所有。
We have identified and synthesized a series of biphenyl-carboxylic acid indanones as allosteric potentiators of the metabotropic glutamate receptor 2. Structure-activity relationship studies directed toward improving the potency and the brain to plasma ratio of the initial lead led to the discovery of 5 and 23 (EC50 = 111 and 5 nM, respectively). (c) 2005 Elsevier Ltd. All rights reserved.