Discovery of TAK-925 as a Potent,Selective, and Brain-Penetrant
Orexin 2 Receptor Agonist |
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| Authors: | Tatsuhiko Fujimoto Kentaro Rikimaru Koichiro Fukuda Hiromichi Sugimoto Kei Masuda Norio Ohyabu Yoshihiro Banno Norihito Tokunaga Tetsuji Kawamoto Yoshihide Tomata Yasumi Kumagai Motoo Iida Yoichi Nagano Mariko Yoneyama-Hirozane Yuji Shimizu Katsunori Sasa Takashi Ishikawa Hiroshi Yukitake Mitsuhiro Ito Kazunobu Aoyama Takahiro Matsumoto |
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| Affiliation: | Research, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan |
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| Abstract: | ![]()
TAK-925, a potent, selective, and brain-penetrant orexin 2 receptor (OX2R) agonist, [methyl (2R,3S)-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. |
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| Keywords: | Orexin 2 receptor agonist OX2R TAK-925 |
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