Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist.
第一作者:
James A,Monn
第一单位:
Discovery Chemistry Research and Technologies, ‡Quantitative Biology, §Structural Biology, ∥Drug Disposition and ⊥Neuroscience Research, Eli Lilly and Company , Lilly Corporate Center, Drop 0510, Indianapolis, Indiana 46285, United States.
作者:
医学主题词
别构调节(Allosteric Regulation);动物(Animals);结合, 竞争性(Binding, Competitive);钙(Calcium);环AMP(Cyclic AMP);狗(Dogs);药物部分激动作用(Drug Partial Agonism);人类(Humans);男(雄)性(Male);小鼠(Mice);模型, 分子(Models, Molecular);运动活动(Motor Activity);诱变, 定点(Mutagenesis, Site-Directed);蛋白质结构, 三级(Protein Structure, Tertiary);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);受体, 亲代谢性谷氨酸盐(Receptors, Metabotropic Glutamate);立体异构现象(Stereoisomerism);三唑类(Triazoles)
DOI
10.1021/acs.jmedchem.5b01124
PMID
26313429
发布时间
2016-11-25
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