Kim, Younghee Son, Jiwon Kim, Juhyeon Baek, Du-Jong Lee, Yong Sup Lim, Eun Jeong Lee, Jae Kyun Pae, Ae Nim Min, Sun-Joon Cho, Yong Seo 2024-01-20T09:34:27Z 2024-01-20T09:34:27Z 2021-09-04 2014-06 0009-2363 https://pubs.kist.re.kr/handle/201004/126765 A series of 2-amino and 2-methoxy quinoline-6-carboxamide derivatives have been synthesized and their metabotropic glutamate receptor type 1 (mGluR1) antagonistic activities were evaluated in a functional cell-based assay. The compound 13c showed the highest potency with IC50 value of 2.16 mu m against mGluR1. Finally, in vivo evaluation of 13c in the rat spinal nerve ligation (SNL) model exhibited weak analgesic effects with regard to both mechanical allodynia and cold allodynia. English PHARMACEUTICAL SOC JAPAN METABOTROPIC GLUTAMATE RECEPTORS GLUTAMATE-RECEPTOR-1 ANTAGONISTS PHARMACOLOGICAL CHARACTERIZATION IN-VITRO DERIVATIVES DISCOVERY MICE PROFILES LY456236 EFFICACY Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain Article 10.1248/cpb.c13-00945 1 CHEMICAL & PHARMACEUTICAL BULLETIN, v.62, no.6, pp.508 - 518 CHEMICAL & PHARMACEUTICAL BULLETIN 62 6 508 518 scie scopus 000336559100002 2-s2.0-84903395807 Chemistry, Medicinal Chemistry, Multidisciplinary Pharmacology & Pharmacy Pharmacology & Pharmacy Chemistry Article METABOTROPIC GLUTAMATE RECEPTORS GLUTAMATE-RECEPTOR-1 ANTAGONISTS PHARMACOLOGICAL CHARACTERIZATION IN-VITRO DERIVATIVES DISCOVERY MICE PROFILES LY456236 EFFICACY glutamate metabotropic glutamate receptor (mGluR) quinoline neuropathic pain spinal nerve ligation (SNL) model