Fused tricyclic mGluR1 antagonists for the treatment of neuropathic pain

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• 作者：Chad E. Bennett^a ; ^{chadbennett3@yahoo.com} ; Duane A. Burnett^a ; William J. Greenlee^a ; Chad E. Knutson^a ; Peter Korakas^a ; Cheng Li^a ; Deen Tulshian^a ; Wen-Lian Wu^a ; Rosalia Bertorelli^b ; Silva Fredduzzi^b ; Mariagrazia Grilli^b ; Gianluca Lozza^b ; Angelo Reggiani^b ; Alessio Veltri^b
• 关键词：mGluR1 (metabotropic glutamate receptor 1) ; Neuropathic pain ; Spinal nerve ligation (SNL) ; Fused tricyclic pyridones ; GPCR
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 出版时间：15 February, 2012
• 年：2012
• 卷：22
• 期：4
• 页码：1575-1578
• 全文大小：877 K

文摘

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.