Discovery of N-[(4R)-6-(4-chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridin-4-yl]-5-methyl-1H-pyrazole-3-carboxamide (MK-5596) as a novel cannabinoid-1 receptor (CB1R) inverse agonist for the treatment of obesity.
作者:
主题词
动物(Animals);减肥药(Anti-Obesity Agents);结合, 竞争性(Binding, Competitive);体重(Body Weight);细胞系(Cell Line);仓鼠亚科(Cricetinae);仓鼠属(Cricetulus);结晶学, X线(Crystallography, X-Ray);狗(Dogs);药物反向激动作用(Drug Inverse Agonism);进食(Eating);快速延迟整流钾通道(Ether-A-Go-Go Potassium Channels);葡糖醛酸甙类(Glucuronides);直鼻猴亚目(Haplorhini);肝细胞(Hepatocytes);人类(Humans);小鼠(Mice);小鼠, 基因敲除(Mice, Knockout);模型, 分子(Models, Molecular);分子构象(Molecular Conformation);吡喃类(Pyrans);吡啶类(Pyridines);大鼠(Rats);受体, 大麻酚, CB1(Receptor, Cannabinoid, CB1);立体异构现象(Stereoisomerism);构效关系(Structure-Activity Relationship)
DOI
10.1021/jm100023j
PMID
20423086
发布时间
2018-12-01
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