Publication Details (including relevant citation information):
Filla, Sandra A., Winter, Mark A., Johnson, Kirk W., Bleakman, David, Bell, Michael G., Bleisch, Thomas J., Castano, Ana M., Clemens-Smith, Amy, del Prado, Miriam, Dieckman, Donna K., Dominguez, Esteban, Escribano, Ana, Ho, Ken H., Hudziak, Kevin J., Katofiasc, Mary A., Martinez-Perez, Jose A., Mateo, Ana, Mathes, Brian M., Mattiuz, Edward L., Ogden, Ann Marie L., Phebus, Lee A., Stack, Douglas R., Stratford, Robert E., Ornstein, Paul L. Journal of Medicinal Chemistry 2002 45 (20) 4383-4386
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.