Bioorganic & medicinal chemistry letters

Indole-and indoline-based kainate analogues with antagonist activity at ionotropic glutamate receptors

X Shou, R Miledi, AR Chamberlin

文献索引：Shou, Xiaohong; Miledi, Ricardo; Chamberlin, A. Richard Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 17 p. 3942 - 3947

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被引用次数: 12

摘要

A conformationally constrained, indole-based kainate analogue was designed based on Gouaux's X-ray structure of kainic acid bound to an iGluR2 (S1S2) construct, a structural model for AMPA/kainate ionotropic glutamate receptors. In contrast to the parent kainic acid, a potent agonist, this compound, along with three structurally related analogues derived from synthetic intermediates, exhibited antagonist behavior towards KAR expressed in ...