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