Indole- and indoline-based kainate analogues with antagonist activity at ionotropic glutamate receptors |
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Authors: | Shou Xiaohong Miledi Ricardo Chamberlin A Richard |
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Institution: | Department of Chemistry, University of California, Irvine, CA 92697, USA. |
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Abstract: | 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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