RO5263397
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| Other names | RO-5263397; Ro 5263397; Ro-5263397 |
| Drug class | Trace amine-associated receptor 1 (TAAR1) partial or full 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 or full agonist which is used in scientific research.[1][2][3][4][5] It is the most well-studied of all of the synthetic TAAR1 ligands.[1] In addition to its use in research, RO5263397 is or was under development for potential clinical use as a medication.[6][7][8]
- ^ a b Wu R, Li JX (December 2021). "Potential of Ligands for Trace Amine-Associated Receptor 1 (TAAR1) in the Management of Substance Use Disorders". CNS Drugs. 35 (12): 1239–1248. doi:10.1007/s40263-021-00871-4. PMC 8787759. PMID 34766253.
- ^ 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.
- ^ "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.
- ^ Revel FG, Moreau JL, Pouzet B, Mory R, Bradaia A, Buchy D, et al. (May 2013). "A new perspective for schizophrenia: TAAR1 agonists reveal antipsychotic- and antidepressant-like activity, improve cognition and control body weight". Mol Psychiatry. 18 (5): 543–556. doi:10.1038/mp.2012.57. PMID 22641180.
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