상세 보기
Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain
- Kim, Younghee;
- Son, Jiwon;
- Kim, Juhyeon;
- Baek, Du-Jong;
- Lee, Yong Sup;
- ... Min, Sun-Joon;
- 외 4명
Citations
WEB OF SCIENCE
5Citations
SCOPUS
5초록
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.
키워드
glutamate; metabotropic glutamate receptor (mGluR); quinoline; neuropathic pain; spinal nerve ligation (SNL) model; METABOTROPIC GLUTAMATE RECEPTORS; GLUTAMATE-RECEPTOR-1 ANTAGONISTS; PHARMACOLOGICAL CHARACTERIZATION; IN-VITRO; DERIVATIVES; DISCOVERY; MICE; PROFILES; LY456236; EFFICACY
- 제목
- Synthesis and Biological Evaluation of 2-Substituted Quinoline 6-Carboxamides as Potential mGluR1 Antagonists for the Treatment of Neuropathic Pain
- 저자
- 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
- 발행일
- 2014-06
- 유형
- Article
- 권
- 62
- 호
- 6
- 페이지
- 508 ~ 518
- 언어
- ENG
- 출판사
- PHARMACEUTICAL SOC JAPAN
- 발행국가
- 일본
- 분량
- 11 페이지
- ISSN
- P 0009-2363