Paul Ornstein - 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.

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      Publication Details (including relevant citation   information):

      Filla, Sandra A, Winter, Mark A, Johnson, Kirk W, Bleakman,   David, Bell, Michael G, Bleisch, Thomas J, Castaño, 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.;

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