Structure-activity relationship studies and discovery of a potent transient receptor potential vanilloid (TRPV1) antagonist 4-[3-chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a clinical candidate for pain management.
第一作者:
Laykea,Tafesse
第一单位:
Discovery Research, Purdue Pharma LP , 6 Cedar Brook Drive, Cranbury, New Jersey 08512, United States.
作者:
主题词
氨基吡啶类(Aminopyridines);镇痛药(Analgesics);动物(Animals);体温(Body Temperature);CHO细胞(CHO Cells);钙(Calcium);辣椒辣素(Capsaicin);仓鼠属(Cricetulus);Freund佐剂(Freund's Adjuvant);神经节, 脊(Ganglia, Spinal);人类(Humans);氢离子浓度(Hydrogen-Ion Concentration);男(雄)性(Male);疼痛(Pain);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);感觉感受器细胞(Sensory Receptor Cells);立体异构现象(Stereoisomerism);构效关系(Structure-Activity Relationship);TRPV阳离子通道(TRPV Cation Channels)
DOI
10.1021/jm500818a
PMID
25057800
发布时间
2014-08-14
- 浏览46
相似文献
- 中文期刊
- 外文期刊
- 学位论文
- 会议论文