Douglas R Stack

Publications (2)10.5 Total impact

• Article: Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain.

  Esteban Dominguez, Smriti Iyengar, Harlan E Shannon, David Bleakman, Andrew Alt, Brian M Arnold, Michael G Bell, Thomas J Bleisch, Jennifer L Buckmaster, Ana M Castano, [......], Ana Mateo, Brian M Mathes, Edward L Mattiuz, Ann Marie L Ogden, Rosa Maria A Simmons, Douglas R Stack, Robert E Stratford, Mark A Winter, Zhipei Wu, Paul L Ornstein
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  ABSTRACT: Amino acids 5 and 7, two potent and selective competitive GluR5 KA receptor antagonists, exhibited high GluR5 receptor affinity over other glutamate receptors. Their ester prodrugs 6 and 8 were orally active in three models of pain: reversal of formalin-induced paw licking, carrageenan-induced thermal hyperalgesia, and capsaicin-induced mechanical hyperalgesia.
  Journal of Medicinal Chemistry 07/2005; 48(13):4200-3. · 5.25 Impact Factor
• Article: 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.

  Sandra A Filla, 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, [......], 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
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  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.
  Journal of Medicinal Chemistry 10/2002; 45(20):4383-6. · 5.25 Impact Factor