Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABA<sub>A</sub>) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.-论文-万方医学网

作者： Michael M,Poe ^[1] ; Kashi Reddy,Methuku ^[1] ; Guanguan,Li ^[1] ; Ashwini R,Verma ^[1] ; Kelly A,Teske ^[1] ; Douglas C,Stafford ^[1] ; Leggy A,Arnold ^[1] ; Jeffrey W,Cramer ^[2] ; Timothy M,Jones ^[2] ; Rok,Cerne ^[2] ; Michael J,Krambis ^[2] ; Jeffrey M,Witkin ^[2] ; Enrique,Jambrina ^[3] ; Sabah,Rehman ^[4] ; Margot,Ernst ^[4] ; James M,Cook ^[1] ; Jeffrey M,Schkeryantz ^[2]

作者单位： Department of Chemistry and Biochemistry and the Milwaukee Institute for Drug Discovery, University of Wisconsin-Milwaukee , Milwaukee, Wisconsin 53201, United States. ^[1] Lilly Research Laboratories, Eli Lilly and Company , Indianapolis, Indiana 42685, United States. ^[2] Lilly Research Laboratories, Eli Lilly and Company , 28108 Alcobendas, Spain. ^[3] Department for Molecular Neurosciences, Medical University of Vienna , 1090 Vienna, Austria. ^[4]

主题词动物(Animals);抗焦虑药(Anti-Anxiety Agents);焦虑(Anxiety);苯二氮|艹卓|类(Benzodiazepines);剂量效应关系, 药物(Dose-Response Relationship, Drug);癫痫(Epilepsy);GABA-A受体拮抗剂(GABA-A Receptor Antagonists);HEK293细胞(HEK293 Cells);人类(Humans);咪唑类(Imidazoles);配体(Ligands);男(雄)性(Male);小鼠(Mice);小鼠, 近交系(Mice, Inbred Strains);分子结构(Molecular Structure);恶唑类(Oxazoles);疼痛(Pain);大鼠(Rats);大鼠, Sprague-Dawley(Rats, Sprague-Dawley);受体, GABA-A(Receptors, GABA-A);构效关系(Structure-Activity Relationship)

DOI 10.1021/acs.jmedchem.6b01332

PMID 27933953

发布时间 2018-11-13

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Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABA<sub>A</sub>) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.

Journal of medicinal chemistry

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Journal of medicinal chemistry

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Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABA<sub>A</sub>) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy.

Journal of medicinal chemistry

相似文献

Journal of medicinal chemistry

相关期刊

检索历史清除