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. 2002 Sep 26;45(20):4383-6.
doi: 10.1021/jm025548q.

Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine

Sandra A Filla  1 , Mark A Winter, Kirk W Johnson, David Bleakman, Michael G Bell, Thomas J Bleisch, Ana M Castaño, Amy Clemens-Smith, Miriam del Prado, Donna K Dieckman, Esteban Dominguez, Ana Escribano, Ken H Ho, Kevin J Hudziak, Mary A Katofiasc, Jose A Martinez-Perez, Ana Mateo, Brian M Mathes, Edward L Mattiuz, Ann Marie L Ogden, Lee A Phebus, Douglas R Stack, Robert E Stratford, Paul L Ornstein
Affiliations

Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine

Sandra A Filla et al. J Med Chem. .

Abstract

Amino diacid 3, a highly selective competitive GluR5 kainate receptor antagonist, exhibited high GluR5 receptor affinity and selectivity over other glutamate receptors. Its diethyl ester prodrug 4 was orally active in two models of migraine: the neurogenic dural plasma protein extravasation model and the nucleus caudalis c-fos expression model. These data suggest that a GluR5 kainate receptor antagonist might be an efficacious antimigraine therapy with a novel mechanism of action.

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