RO5263397

RO5263397
Clinical data
Other names	RO-5263397; Ro 5263397; Ro-5263397
Drug class	Trace amine-associated receptor 1 (TAAR1) agonist
Identifiers
	IUPAC name (4S)-4-(3-fluoro-2-methylphenyl)-4,5-dihydro-1,3-oxazol-2-amine;
CAS Number	1357266-05-7;
PubChem CID	56835991;
ChemSpider	35523070;
UNII	Y2P4KD8GDR;
ChEMBL	ChEMBL3781694;
Chemical and physical data
Formula	C10H11FN2O
Molar mass	194.209 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES CC1=C(C=CC=C1F)[C@H]2COC(=N2)N;
	InChI InChI=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; Key: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 EC₅₀Tooltip half-maximal effective concentration values are 0.12 nM for the mouse TAAR1 (mTAAR1), 35 nM for the rat TAAR1 (rTAAR1), and 17 to 85 nM for the human TAAR1 (hTAAR1).^[2] Similarly to other TAAR1 agonists like RO5166017 and RO5256390, RO5263397 shows aversive effects in animals.^[3]^[4]

References

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

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