Fujimoto Tatsuhiko, Rikimaru Kentaro, Fukuda Koichiro, Sugimoto Hiromichi, Masuda Kei, Ohyabu Norio, Banno Yoshihiro, Tokunaga Norihito, Kawamoto Tetsuji, Tomata Yoshihide, Kumagai Yasumi, Iida Motoo, Nagano Yoichi, Yoneyama-Hirozane Mariko, Shimizu Yuji, Sasa Katsunori, Ishikawa Takashi, Yukitake Hiroshi, Ito Mitsuhiro, Aoyama Kazunobu, Matsumoto Takahiro
Research, Takeda Pharmaceutical Company Limited, 26-1, Muraoka-Higashi 2-Chome, Fujisawa, Kanagawa 251-8555, Japan.
ACS Med Chem Lett. 2022 Feb 4;13(3):457-462. doi: 10.1021/acsmedchemlett.1c00626. eCollection 2022 Mar 10.
TAK-925, a potent, selective, and brain-penetrant orexin 2 receptor (OX2R) agonist, [methyl (2,3)-3-((methylsulfonyl)amino)-2-(((-4-phenylcyclohexyl)oxy)methyl)piperidine-1-carboxylate, ], was identified through the optimization of compound , which was discovered by a high throughput screening (HTS) campaign. Subcutaneous administration of compound produced wake-promoting effects in mice during the sleep phase. Compound (TAK-925) is being developed for the treatment of narcolepsy and other related disorders.
TAK-925，一种强效、选择性且可穿透血脑屏障的食欲素2受体（OX2R）激动剂，[（2,3）-3-（（甲基磺酰基）氨基）-2-（（（-4-苯基环己基）氧基）甲基）哌啶-1-羧酸甲酯]，是通过对化合物进行优化而鉴定出来的，该化合物是通过高通量筛选（HTS）活动发现的。在睡眠阶段皮下注射该化合物可在小鼠中产生促觉醒作用。化合物（TAK-925）正在开发用于治疗发作性睡病和其他相关疾病。
