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XB-ART-1660
Bioorg Med Chem Lett 2005 Sep 01;1517:3942-7. doi: 10.1016/j.bmcl.2005.05.098.
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Indole- and indoline-based kainate analogues with antagonist activity at ionotropic glutamate receptors.

Shou X , Miledi R , Chamberlin AR .


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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 oocytes, a result that is rationalized by molecular modeling studies.

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Species referenced: Xenopus
Genes referenced: hsd17b12