1. Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.
- Author
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Fujimoto T, Rikimaru K, Fukuda K, Sugimoto H, Masuda K, Ohyabu N, Banno Y, Tokunaga N, Kawamoto T, Tomata Y, Kumagai Y, Iida M, Nagano Y, Yoneyama-Hirozane M, Shimizu Y, Sasa K, Ishikawa T, Yukitake H, Ito M, Aoyama K, and Matsumoto T
- Abstract
TAK-925, a potent, selective, and brain-penetrant orexin 2 receptor (OX2R) agonist, [methyl (2 R ,3 S )-3-((methylsulfonyl)amino)-2-((( cis -4-phenylcyclohexyl)oxy)methyl)piperidine-1-carboxylate, 16 ], was identified through the optimization of compound 2 , which was discovered by a high throughput screening (HTS) campaign. Subcutaneous administration of compound 16 produced wake-promoting effects in mice during the sleep phase. Compound 16 (TAK-925) is being developed for the treatment of narcolepsy and other related disorders., Competing Interests: The authors declare no competing financial interest., (© 2022 The Authors. Published by American Chemical Society.)
- Published
- 2022
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