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Two Prodrugs of Potent and Selective GluR5 Kainate Receptor Antagonists Actives in Three Animal Models of Pain

2005; American Chemical Society; Volume: 48; Issue: 13 Linguagem: Inglês

10.1021/jm0491952

1520-4804

Esteban Domı́nguez, Smriti Iyengar, Harlan E. Shannon, David Bleakman, Andrew Alt, Brian M. Arnold, Michael G. Bell, Thomas J. Bleisch, Jennifer L. Buckmaster, Ana M. Castaño‐León, Miriam Del Prado, Ana Escribano, Sandra Filla, Ken H. Ho, Kevin J. Hudziak, Carrie K. Jones, José Antonio Martínez-Pérez, 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,

Bioactive Compounds and Antitumor Agents

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.