Son, Myung-Hee Kim, Ji Young Lim, Eun Jeong Baek, Du-Jong Choi, Kihang Lee, Jae Kyun Pae, Ae Nim Min, Sun-Joon Cho, Yong Seo 2024-01-20T12:34:41Z 2024-01-20T12:34:41Z 2021-09-01 2013-03-01 0960-894X https://pubs.kist.re.kr/handle/201004/128257 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. (c) 2012 Elsevier Ltd. All rights reserved. English Pergamon Press Ltd. METABOTROPIC GLUTAMATE RECEPTORS RAT MODEL 2-METHYL-6-(PHENYLETHYNYL)-PYRIDINE MPEP ALLOSTERIC MODULATORS POTENT ALLODYNIA COGNITION DISEASE ANXIETY Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain Article 10.1016/j.bmcl.2012.12.056 1 Bioorganic & Medicinal Chemistry Letters, v.23, no.5, pp.1472 - 1476 Bioorganic & Medicinal Chemistry Letters 23 5 1472 1476 scie scopus 000314693400064 2-s2.0-84873744551 Chemistry, Medicinal Chemistry, Organic Pharmacology & Pharmacy Chemistry Article METABOTROPIC GLUTAMATE RECEPTORS RAT MODEL 2-METHYL-6-(PHENYLETHYNYL)-PYRIDINE MPEP ALLOSTERIC MODULATORS POTENT ALLODYNIA COGNITION DISEASE ANXIETY Metabotropic glutamate receptor Antagonist Quinoline Sonogashira reaction Neuropathic pain