Paul Ornstein - Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycarbonylimidazol-1-ylmethyl)decahydroisoquinoline-3- carboxylic ester: A prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine

Document created by Paul Ornstein on Jan 17, 2017
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  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.

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