Identification and in Vivo Evaluation of Liver X Receptor β‑Selective Agonists for the Potential Treatment of Alzheimer’s Disease

Herein, we describe the development of a functionally selective liver X receptor β (LXRβ) agonist series optimized for Emax selectivity, solubility, and physical properties to allow efficacy and safety studies in vivo. Compound 9 showed central pharmacodynamic effects in rodent models, evidenced by...

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Veröffentlicht in:	Journal of medicinal chemistry 2016-04, Vol.59 (7), p.3489-3498
Hauptverfasser:	Stachel, Shawn J, Zerbinatti, Celina, Rudd, Michael T, Cosden, Mali, Suon, Sokreine, Nanda, Kausik K, Wessner, Keith, DiMuzio, Jillian, Maxwell, Jill, Wu, Zhenhua, Uslaner, Jason M, Michener, Maria S, Szczerba, Peter, Brnardic, Edward, Rada, Vanessa, Kim, Yuntae, Meissner, Robert, Wuelfing, Peter, Yuan, Yang, Ballard, Jeanine, Holahan, Marie, Klein, Daniel J, Lu, Jun, Fradera, Xavier, Parthasarathy, Gopal, Uebele, Victor N, Chen, Zhongguo, Li, Yingjie, Li, Jian, Cooke, Andrew J, Bennett, D. Jonathan, Bilodeau, Mark T, Renger, John
Format:	Artikel
Sprache:	eng
Schlagworte:	60 APPLIED LIFE SCIENCES agonists Alzheimer Disease - drug therapy Amyloid beta-Peptides - cerebrospinal fluid Animals Apolipoproteins E - cerebrospinal fluid ATP-Binding Cassette Transporters - metabolism Benzamides - chemistry Benzamides - pharmacology Brain - drug effects Brain - metabolism central nervous system Dogs Hep G2 Cells Humans INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY lipids Lipids - analysis Liver - drug effects Liver - metabolism Liver X Receptors Locomotion - drug effects Macaca mulatta Madin Darby Canine Kidney Cells Mice Mice, Transgenic Orphan Nuclear Receptors - agonists peptides and proteins Piperidines - chemistry Piperidines - pharmacology rodent models
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