| Identification | Back Directory | [Name]
1-Piperidinecarboxylic acid, 3-[(methylsulfonyl)amino]-2-[[(cis-4-phenylcyclohexyl)oxy]methyl]-, methyl ester, (2R,3S)- | [CAS]
2114324-48-8 | [Synonyms]
Danavorexton
1-Piperidinecarboxylic acid, 3-[(methylsulfonyl)amino]-2-[[(cis-4-phenylcyclohexyl)oxy]methyl]-, methyl ester, (2R,3S)- | [Molecular Formula]
C21H32N2O5S | [MOL File]
2114324-48-8.mol | [Molecular Weight]
424.55 |
| Hazard Information | Back Directory | [Uses]
Danavorexton (TAK-925) is an orexin receptor agonist with brain permeability. Danavorexton induces a physiological pattern of OX2R activation in vitro to wake up sleepy mice and improve sleepiness symptoms[1][2][3][4]. | [in vivo]
Danavorexton (1, 10 mg/kg or 1, 3 mg/kg, subcutaneous injection) dose-dependent enhanced arousal in common marmosets and cynomolgus monkeys[2].
| Animal Model: | Common marmosets and cynomolgus monkeys models[2] | | Dosage: | 1, 10 mg/kg (1, 3 mg/kg) | | Administration: | s.c. | | Result: | Decreased SWS I (Sleeping With Sirens I), SWS II (Sleeping With Sirens II) and REM (Rapid Eye Movement) sleep time. |
| [References]
[1] International Nonproprietary Names for Pharmaceutical Substances (INN). WHO Drug Information, Vol. 34, No. 2, 2020.
[2] Evans R, et al. Orexin 2 receptor-selective agonist danavorexton (TAK-925) promotes wakefulness in non-human primates and healthy individuals. J Sleep Res. 2023 Oct;32(5):e13878 DOI:10.1111/jsr.13878
[3] Ishikawa T, et al. Danavorexton, a selective orexin 2 receptor agonist, provides a symptomatic improvement in a narcolepsy mouse model. Pharmacol Biochem Behav. 2022 Oct;220:173464. DOI:10.1016/j.pbb.2022.173464
[4] Fujimoto T, et al. 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 |
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