2. Academic Validation
  3. Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist

Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist

  • ACS Med Chem Lett. 2022 Feb 4;13(3):457-462. doi: 10.1021/acsmedchemlett.1c00626.
Tatsuhiko Fujimoto 1,  Kentaro Rikimaru 1,  Koichiro Fukuda 1,  Hiromichi Sugimoto 1,  Kei Masuda 1,  Norio Ohyabu 1,  Yoshihiro Banno 1,  Norihito Tokunaga 1,  Tetsuji Kawamoto 1,  Yoshihide Tomata 1,  Yasumi Kumagai 1,  Motoo Iida 1,  Yoichi Nagano 1,  Mariko Yoneyama-Hirozane 1,  Yuji Shimizu 1,  Katsunori Sasa 1,  Takashi Ishikawa 1,  Hiroshi Yukitake 1,  Mitsuhiro Ito 1,  Kazunobu Aoyama 1,  Takahiro Matsumoto 1
Affiliations

Affiliation

  • 1 Research, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
PMID: 35295087 DOI: 10.1021/acsmedchemlett.1c00626
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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