Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Chad E. Bennett; Duane A. Burnett; William J. Greenlee; Chad E. Knutson; Peter Korakas; Cheng Li; Deen Tulshian; Wen Lian Wu; Rosalia Bertorelli; Silva Fredduzzi; Mariagrazia Grilli; Gianluca Lozza; Angelo Reggiani; Alessio Veltri

doi:10.1016/j.bmcl.2011.12.131

Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Chad E. Bennett
, Duane A. Burnett
, William J. Greenlee
, Chad E. Knutson
, Peter Korakas
, Cheng Li
, Deen Tulshian
, Wen Lian Wu
, Rosalia Bertorelli
, Silva Fredduzzi
, Mariagrazia Grilli
, Gianluca Lozza
, Angelo Reggiani
, Alessio Veltri

Risultato della ricerca: Contributo su rivista › Articolo in rivista › peer review

Abstract

A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test.

Lingua originale	Inglese
pagine (da-a)	1575-1578
Numero di pagine	4
Rivista	Bioorganic and Medicinal Chemistry Letters
Volume	22
Numero di pubblicazione	4
DOI	https://doi.org/10.1016/j.bmcl.2011.12.131
Stato di pubblicazione	Pubblicato - 15 feb 2012
Pubblicato esternamente	Sì

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10.1016/j.bmcl.2011.12.131

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Bennett, C. E., Burnett, D. A., Greenlee, W. J., Knutson, C. E., Korakas, P., Li, C., Tulshian, D., Wu, W. L., Bertorelli, R., Fredduzzi, S., Grilli, M., Lozza, G., Reggiani, A., & Veltri, A. (2012). Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain. Bioorganic and Medicinal Chemistry Letters, 22(4), 1575-1578. https://doi.org/10.1016/j.bmcl.2011.12.131

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abstract = "A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test.",

keywords = "Fused tricyclic pyridones, GPCR, MGluR1 (metabotropic glutamate receptor 1), Neuropathic pain, Spinal nerve ligation (SNL)",

author = "Bennett, \{Chad E.\} and Burnett, \{Duane A.\} and Greenlee, \{William J.\} and Knutson, \{Chad E.\} and Peter Korakas and Cheng Li and Deen Tulshian and Wu, \{Wen Lian\} and Rosalia Bertorelli and Silva Fredduzzi and Mariagrazia Grilli and Gianluca Lozza and Angelo Reggiani and Alessio Veltri",

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doi = "10.1016/j.bmcl.2011.12.131",

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AU - Bennett, Chad E.

AU - Burnett, Duane A.

AU - Greenlee, William J.

AU - Knutson, Chad E.

AU - Korakas, Peter

AU - Li, Cheng

AU - Tulshian, Deen

AU - Wu, Wen Lian

AU - Bertorelli, Rosalia

AU - Fredduzzi, Silva

AU - Grilli, Mariagrazia

AU - Lozza, Gianluca

AU - Reggiani, Angelo

AU - Veltri, Alessio

PY - 2012/2/15

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AB - A series of fused tricyclic mGluR1 antagonists containing a pyridone ring were synthesized. In vitro, these antagonists were potent against both human and rat isozymes, as well as selective for inhibiting mGluR1 over mGluR5. When dosed orally, several examples were active in vivo in a rat SNL test.

KW - Fused tricyclic pyridones

KW - GPCR

KW - MGluR1 (metabotropic glutamate receptor 1)

KW - Neuropathic pain

KW - Spinal nerve ligation (SNL)

UR - https://www.scopus.com/pages/publications/84862826031

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DO - 10.1016/j.bmcl.2011.12.131

M3 - Article

SN - 0960-894X

VL - 22

SP - 1575

EP - 1578

JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 4

ER -

Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

Abstract

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