Ethyl (3 S ,4a R ,6 S ,8a R )-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
2002; American Chemical Society; Volume: 45; Issue: 20 Linguagem: Inglês
10.1021/jm025548q
ISSN1520-4804
AutoresSandra Filla, Mark A. Winter, Kirk W. Johnson, David Bleakman, Michael G. Bell, Thomas J. Bleisch, Ana M. Castaño‐León, Amy Clemens‐Smith, Miriam Del Prado, Donna K. Dieckman, Esteban Domı́nguez, Ana Escribano, Ken H. Ho, Kevin J. Hudziak, Mary A. Katofiasc, José Antonio Martínez-Pérez, Ana Mateo, Brian M. Mathes, Edward L. Mattiuz, Ann Marie L. Ogden, Lee A. Phebus, Douglas R. Stack, Robert E. Stratford, Paul L. Ornstein,
Tópico(s)Neuroscience and Neuropharmacology Research
ResumoAmino 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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