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, Miriam Del Prado, Ana Escribano, Sandra A. Filla, Ken H. Ho, Kevin J. Hudziak, Carrie K. Jones, Jose A. Martinez-Perez, Ana Mateo, Brian M. Mathes, Edward L. MattiuzAnn Marie L. Ogden, Rosa Maria A. Simmons, Douglas R. Stack, Robert E. Stratford, Mark A. Winter, Zhipei Wu, Paul L. Ornsteint

Research output: Contribution to journalArticle

31 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)4200-4203
Number of pages4
JournalJournal of Medicinal Chemistry
Volume48
Issue number13
DOIs
StatePublished - Jun 30 2005
Externally publishedYes

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Dominguez, E., Iyengar, S., Shannon, H. E., Bleakman, D., Alt, A., Arnold, B. M., Bell, M. G., Bleisch, T. J., Buckmaster, J. L., Castano, A. M., Del Prado, M., Escribano, A., Filla, S. A., Ho, K. H., Hudziak, K. J., Jones, C. K., Martinez-Perez, J. A., Mateo, A., Mathes, B. M., ... Ornsteint, P. L. (2005). Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. Journal of Medicinal Chemistry, 48(13), 4200-4203. https://doi.org/10.1021/jm0491952