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Discovery of TAK-925 as a Potent, Selective, and Brain-Penetrant Orexin 2 Receptor Agonist.
- Source :
-
ACS medicinal chemistry letters [ACS Med Chem Lett] 2022 Feb 04; Vol. 13 (3), pp. 457-462. Date of Electronic Publication: 2022 Feb 04 (Print Publication: 2022). - Publication Year :
- 2022
-
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.<br />Competing Interests: The authors declare no competing financial interest.<br /> (© 2022 The Authors. Published by American Chemical Society.)
Details
- Language :
- English
- ISSN :
- 1948-5875
- Volume :
- 13
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- ACS medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 35295087
- Full Text :
- https://doi.org/10.1021/acsmedchemlett.1c00626