Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588023 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
We described here the synthesis and biological evaluation of mGluR5 antagonists containing a quinoline ring structure. Using intracellular calcium mobilization assay (FDSS assay), we identified compound 5n, showing high inhibitory activity against mGluR5. In addition, it was found that compound 5n has excellent stability profile. Finally, this compound exhibited favorable analgesic effects in spinal nerve ligation model of neuropathic pain, which is comparable to gabapentin.
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Authors
Myung-Hee Son, Ji Young Kim, Eun Jeong Lim, Du-Jong Baek, Kihang Choi, Jae Kyun Lee, Ae Nim Pae, Sun-Joon Min, Yong Seo Cho,