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 Stratford Jr., Mark A. Winter, Zhipei Wu, Paul L. Ornsteint

Research output: Contribution to journalArticle

31 Citations (Scopus)

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

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Hyperalgesia
Prodrugs
Animal Models
Pain
Carrageenan
Capsaicin
Glutamate Receptors
Formaldehyde
Esters
Amino Acids
Gluk1 kainate receptor

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

Cite this

Dominguez, E., Iyengar, S., Shannon, H. E., Bleakman, D., Alt, A., Arnold, 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

Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. / Dominguez, Esteban; Iyengar, Smriti; Shannon, Harlan E.; Bleakman, David; Alt, Andrew; Arnold, Brian M.; Bell, Michael G.; Bleisch, Thomas J.; Buckmaster, Jennifer L.; Castano, Ana M.; Del Prado, Miriam; Escribano, Ana; Filla, Sandra A.; Ho, Ken H.; Hudziak, Kevin J.; Jones, Carrie K.; Martinez-Perez, Jose A.; Mateo, Ana; Mathes, Brian M.; Mattiuz, Edward L.; Ogden, Ann Marie L.; Simmons, Rosa Maria A.; Stack, Douglas R.; Stratford Jr., Robert; Winter, Mark A.; Wu, Zhipei; Ornsteint, Paul L.

In: Journal of Medicinal Chemistry, Vol. 48, No. 13, 30.06.2005, p. 4200-4203.

Research output: Contribution to journalArticle

Dominguez, E, Iyengar, S, Shannon, HE, Bleakman, D, Alt, A, Arnold, BM, Bell, MG, Bleisch, TJ, Buckmaster, JL, Castano, AM, Del Prado, M, Escribano, A, Filla, SA, Ho, KH, Hudziak, KJ, Jones, CK, Martinez-Perez, JA, Mateo, A, Mathes, BM, Mattiuz, EL, Ogden, AML, Simmons, RMA, Stack, DR, Stratford Jr., R, Winter, MA, Wu, Z & Ornsteint, PL 2005, 'Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain', Journal of Medicinal Chemistry, vol. 48, no. 13, pp. 4200-4203. https://doi.org/10.1021/jm0491952
Dominguez, Esteban ; Iyengar, Smriti ; Shannon, Harlan E. ; Bleakman, David ; Alt, Andrew ; Arnold, Brian M. ; Bell, Michael G. ; Bleisch, Thomas J. ; Buckmaster, Jennifer L. ; Castano, Ana M. ; Del Prado, Miriam ; Escribano, Ana ; Filla, Sandra A. ; Ho, Ken H. ; Hudziak, Kevin J. ; Jones, Carrie K. ; Martinez-Perez, Jose A. ; Mateo, Ana ; Mathes, Brian M. ; Mattiuz, Edward L. ; Ogden, Ann Marie L. ; Simmons, Rosa Maria A. ; Stack, Douglas R. ; Stratford Jr., Robert ; Winter, Mark A. ; Wu, Zhipei ; Ornsteint, Paul L. / Two prodrugs of potent and selective GluR5 kainate receptor antagonists actives in three animal models of pain. In: Journal of Medicinal Chemistry. 2005 ; Vol. 48, No. 13. pp. 4200-4203.
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AU - Dominguez, Esteban

AU - Iyengar, Smriti

AU - Shannon, Harlan E.

AU - Bleakman, David

AU - Alt, Andrew

AU - Arnold, Brian M.

AU - Bell, Michael G.

AU - Bleisch, Thomas J.

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AU - Castano, Ana M.

AU - Del Prado, Miriam

AU - Escribano, Ana

AU - Filla, Sandra A.

AU - Ho, Ken H.

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AU - Jones, Carrie K.

AU - Martinez-Perez, Jose A.

AU - Mateo, Ana

AU - Mathes, Brian M.

AU - Mattiuz, Edward L.

AU - Ogden, Ann Marie L.

AU - Simmons, Rosa Maria A.

AU - Stack, Douglas R.

AU - Stratford Jr., Robert

AU - Winter, Mark A.

AU - Wu, Zhipei

AU - Ornsteint, Paul L.

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