Discovery of cis-N-(1-(4-(methylamino)cyclohexyl)indolin-6-yl)thiophene-2-carboximidamide: a 1,6-disubstituted indoline derivative as a highly selective inhibitor of human neuronal nitric oxide synthase (nNOS) without any cardiovascular liabilities.
第一作者:
Subhash C,Annedi
第一单位:
NeurAxon Inc. , 2395 Speakman Drive, Suite 1001, Mississauga, Ontario L5K 1B3, Canada.
作者:
主题词
镇痛药(Analgesics);动物(Animals);动脉(Arteries);心血管系统(Cardiovascular System);快速延迟整流钾通道(Ether-A-Go-Go Potassium Channels);HEK293细胞(HEK293 Cells);高通量筛选分析(High-Throughput Screening Assays);人类(Humans);吲哚类(Indoles);神经痛(Neuralgia);一氧化氮合酶Ⅰ型(Nitric Oxide Synthase Type I);一氧化氮合酶Ⅱ型(Nitric Oxide Synthase Type II);一氧化氮合酶Ⅲ型(Nitric Oxide Synthase Type III);膜片钳术(Patch-Clamp Techniques);大鼠(Rats);立体异构现象(Stereoisomerism);构效关系(Structure-Activity Relationship);噻吩类(Thiophenes);血管阻力(Vascular Resistance);血管收缩(Vasoconstriction)
DOI
10.1021/jm201564u
PMID
22175766
发布时间
2016-11-25
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