RO5263397 is a potent, selective, and orally available TAAR1 agonist, with EC50s of 17 and 35 nM for human TAAR1 and rat TAAR1, respectively. RO5263397 regulates wakefulness and EEG spectral composition. Antidepressant-like effect[2].In Vivo: RO5263397 (0.1-1.0?mg/kg; p.o.; dosing at the mid-light phase (ZT6)) increased wake time at 0.3 and 1?mg/kg[2].
RO5263397 (0.3 and 1.0?mg/kg; p.o.) decreases 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.