RO5263397
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(Redirected from Ro-5263397)
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Other names | RO-5263397; Ro 5263397; Ro-5263397 |
Drug class | Trace amine-associated receptor 1 (TAAR1) agonist |
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Formula | C10H11FN2O |
Molar mass | 194.209 g·mol−1 |
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RO5263397, or RO-5263397, is a trace amine-associated receptor 1 (TAAR1) partial agonist which is used in scientific research.[1][2] Its EC50 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]- ^ 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.
- ^ 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.