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  • Ethyl (3S,4aR,6S,8aR)-6-(4-...
    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
    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, 09/2002, Letnik: 45, Številka: 20
    Journal Article

    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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