ro5263397

RO5263397是一种 TAAR1特异性激动剂，具有口服活性，被用于抗抑郁研究。它还被发现作为环氧化酶-2 (COX-2)的抑制剂，参与前列腺素的合成。

(4R)-4-(3-Fluoro-2-methylphenyl)-4,5-dihydro-2-oxazolamin 对 TRACE AMINE ASSOCIATED RECEPTOR (TAAR 1)具有活性，EC50为0.017 μM，可用来研究神经系统疾病。

Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 |Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID:26985297 |Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID:27658486