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Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain
- Authors
- 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
- Issue Date
- Jun-2014
- Publisher
- Pharmaceutical Society of Japan
- Keywords
- glutamate; metabotropic glutamate receptor (mGluR); quinoline; neuropathic pain; spinal nerve ligation (SNL) model
- Citation
- Chemical and Pharmaceutical Bulletin, v.62, no.6, pp.508 - 518
- Indexed
- SCIE
SCOPUS
- Journal Title
- Chemical and Pharmaceutical Bulletin
- Volume
- 62
- Number
- 6
- Start Page
- 508
- End Page
- 518
- ISSN
- 0009-2363
- Abstract
- 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.
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Related Researcher
- Min, Sun Joon
- COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY (DEPARTMENT OF CHEMICAL AND MOLECULAR ENGINEERING)