RO5263397 explained

Class:	Trace amine-associated receptor 1 (TAAR1) agonist
Cas Number:	1357266-05-7
Pubchem:	56835991
Chemspiderid:	35523070
Unii:	Y2P4KD8GDR
Chembl:	3781694
Synonyms:	RO-5263397; Ro 5263397; Ro-5263397
Iupac Name:	(4S)-4-(3-fluoro-2-methylphenyl)-4,5-dihydro-1,3-oxazol-2-amine
C:	10
H:	11
F:	1
N:	2
O:	1
Smiles:	CC1=C(C=CC=C1F)[C@H]2COC(=N2)N
Stdinchi:	1S/C10H11FN2O/c1-6-7(3-2-4-8(6)11)9-5-14-10(12)13-9/h2-4,9H,5H2,1H3,(H2,12,13)/t9-/m1/s1
Stdinchikey:	IOHOUWIYOVWGHV-SECBINFHSA-N

RO5263397, or RO-5263397, is a trace amine-associated receptor 1 (TAAR1) partial agonist which is used in scientific research.^{[1] [2]} Its values are 0.12nM for the mouse TAAR1 (mTAAR1), 35nM for the rat TAAR1 (rTAAR1), and 17 to 85nM for the human TAAR1 (hTAAR1). Similarly to other TAAR1 agonists like RO5166017 and RO5256390, RO5263397 shows aversive effects in animals.^{[3] [4]}

Notes and References

1. Schwartz MD, Canales JJ, Zucchi R, Espinoza S, Sukhanov I, Gainetdinov RR . Trace amine-associated receptor 1: a multimodal therapeutic target for neuropsychiatric diseases . Expert Opinion on Therapeutic Targets . 22 . 6 . 513–526 . June 2018 . 29798691 . 10.1080/14728222.2018.1480723 . 11568/930006 . free .
2. Web site: RO 5263397 hydrochloride Supplier . Tocris Bioscience . 29 October 2024 . RO 5263397 hydrochloride is a 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..
3. Shabani S, Houlton S, Ghimire B, Tonello D, Reed C, Baba H, Aldrich S, Phillips TJ . Robust aversive effects of trace amine-associated receptor 1 activation in mice . Neuropsychopharmacology . 48 . 10 . 1446–1454 . September 2023 . 37055488 . 10425385 . 10.1038/s41386-023-01578-4 .
4. Liu J, Wu R, Johnson B, Zhang Y, Zhu Q, Li JX . Selective TAAR1 agonists induce conditioned taste aversion . Psychopharmacology . 239 . 10 . 3345–3353 . October 2022 . 36056214 . 10.1007/s00213-022-06222-5 .