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RO5263397

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RO5263397
Clinical data
Other namesRO-5263397; Ro 5263397; Ro-5263397
Drug classTrace amine-associated receptor 1 (TAAR1) agonist
Identifiers
  • (4S)-4-(3-fluoro-2-methylphenyl)-4,5-dihydro-1,3-oxazol-2-amine
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC10H11FN2O
Molar mass194.209 g·mol−1
3D model (JSmol)
  • CC1=C(C=CC=C1F)[C@H]2COC(=N2)N
  • 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

[edit]
  1. ^ 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. hdl:11568/930006. PMID 29798691.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.