| Description | RO5263397 is a TAAR1 specific agonist with oral activity that has been used in antidepressant studies. It has also been found to act as an inhibitor of the enzyme cyclooxygenase-2 (COX-2), which is involved in the synthesis of prostaglandins. |
| In vivo | Dosing at the mid-light phase (ZT6)(RO5263397) increased wake time at 0.3 and 1 mg/kg. RO5263397 ecreases NREM time in WT mice. RO5263397 (0.3 and 1.0 mg/kg; p.o.; in OE mice) powerfully increases W time in OE mice for 5-6 h. NREM sleep is suppressed for 4-6 h and REM sleep is almost completely suppressed for 6 h after all doses of RO5263397[3]. |
| molecular weight | 194.21 |
| Molecular formula | C10H11FN2O |
| CAS | 1357266-05-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 234.0 mg/mL (1204.9 mM), Sonication is recommended. |
| References | 1. Galley G, et al. Discovery and Characterization of 2-Aminooxazolines as Highly Potent, Selective, and Orally Active TAAR1 Agonists.ACS Med Chem Lett. 2015 Dec 30;7(2):192-7. 2. Schwartz MD, et al. Trace Amine-Associated Receptor 1 Regulates Wakefulness and EEG Spectral Composition.Neuropsychopharmacology. 2017 May;42(6):1305-1314. 3. Espinoza S, et al. Biochemical and Functional Characterization of the Trace Amine-Associated Receptor 1 (TAAR1) Agonist RO5263397.Front Pharmacol. 2018 Jun 21;9:645. |