Indole- and indoline-based kainate analogues with ...[Bioorg Med Chem Lett. 2005]

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1: Bioorg Med Chem Lett. 2005 Sep 1;15(17):3942-7. Links

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

Shou X, Miledi R, Chamberlin AR.

Department of Chemistry, University of California, Irvine, CA 92697, USA.

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.

PMID: 16005214 [PubMed - indexed for MEDLINE]

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

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