See today's edition of
DailyUpdates in your
therapeutic area
Search all articles

Keywords:

Boolean terms AND, OR, NOT can be used. Phrases should be entered within quotes. For wildcards use an *

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

Bioorganic & medicinal chemistry letters 2005 Sep 1; 15(17):3942-7

Link to PubMed abstract

Shou X X, Miledi R R, Chamberlin A 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.