| Literature DB >> 12238915 |
Sandra A Filla1, 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.
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.Entities:
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Year: 2002 PMID： 12238915 DOI： 10.1021/jm025548q
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446