Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain |
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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 |
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| Institution: | 1. Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology (KIST), Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791, Republic of Korea;2. Department of Chemistry, College of Natural Sciences, Sangmyung University, Hong-ji moon 2-gil 20, Jongno-gu, Seoul 110-743, Republic of Korea;3. Department of Chemistry, Korea University, Seoul 136-701, Republic of Korea;4. Biomolecular Science, University of Science and Technology (UST), 176 Gajung-dong, 217 Gajungro, Yuseong-gu, Daejeon 305-333, Republic of Korea |
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| 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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