期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 22, 期 4, 页码 1575-1578出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2011.12.131
关键词
mGluR1 (metabotropic glutamate receptor 1); Neuropathic pain; Spinal nerve ligation (SNL); Fused tricyclic pyridones; GPCR
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. (C) 2012 Elsevier Ltd. All rights reserved.
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