title: Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain.
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.
authors: Center for Neuro-Medicine, Brain Science Institute, Korea Institute of Science and Technology, Hwarangno 14-gil 5, Seongbuk-gu, Seoul 136-791, Republic of Korea.
authors: Myung-Hee
authors: MH
authors: Son
authors: Ji Young
authors: JY
authors: Kim
authors: Eun Jeong
authors: EJ
authors: Lim
authors: Du-Jong
authors: DJ
authors: Baek
authors: Kihang
authors: K
authors: Choi
authors: Jae Kyun
authors: JK
authors: Lee
authors: Ae Nim
authors: AN
authors: Pae
authors: Sun-Joon
authors: SJ
authors: Min
authors: Yong Seo
authors: YS
authors: Cho
mesh_terms: D000114:Acetylene / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D057809:HEK293 Cells; D006801:Humans; D009437:Neuralgia / Q000188:drug therapy*; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D064529:Receptor, Metabotropic Glutamate 5 / Q000037:antagonists & inhibitors*
chemical_list: D011804:Quinolines; D064529:Receptor, Metabotropic Glutamate 5; D000114:Acetylene