For research use only. Not for therapeutic Use.
RO5263397 is a selective TAAR 1 agonist. RO5263397 was efficacious in reducing cocaine-mediated behaviors. RO5263397 dose-dependently prevented cocaine-induced lowering of ICSS thresholds. TAAR1 stimulation effectively suppresses the rewarding and reinforcing effects of cocaine in self-administration and ICSS models, supporting the candidacy of TAAR1 as a drug discovery target for cocaine addiction.
| Catalog Number | R024741 |
| CAS Number | 1357266-05-7 |
| Synonyms | (4S)-4-(3-Fluoro-2-methylphenyl)-4,5-dihydro-2-oxazolamine |
| Molecular Formula | C10H11FN2O |
| Purity | ≥95% |
| Target | Trace Amine-associated Receptor (TAAR) |
| Storage | Store at -20°C |
| IUPAC Name | (4S)-4-(3-fluoro-2-methylphenyl)-4,5-dihydro-1,3-oxazol-2-amine |
| 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 |
| InChIKey | IOHOUWIYOVWGHV-SECBINFHSA-N |
| SMILES | CC1=C(C=CC=C1F)C2COC(=N2)N |
| Reference | </br>1: Pei Y, Mortas P, Hoener MC, Canales JJ. Selective activation of the trace</br> amine-associated receptor 1 decreases cocaine/’s reinforcing efficacy and prevents</br> cocaine-induced changes in brain reward thresholds. Prog Neuropsychopharmacol</br> Biol Psychiatry. 2015 Dec 3;63:70-5. doi: 10.1016/j.pnpbp.2015.05.014. Epub 2015 </br> Jun 3. PubMed PMID: 26048337.</br>2: Jing L, Zhang Y, Li JX. Effects of the trace amine associated receptor 1</br> agonist RO5263397 on abuse-related behavioral indices of methamphetamine in rats.</br> Int J Neuropsychopharmacol. 2014 Oct 31;18(4). pii: pyu060. doi:</br> 10.1093/ijnp/pyu060. PubMed PMID: 25522401; PubMed Central PMCID: PMC4360231.</br>3: Fowler S, Kletzl H, Finel M, Manevski N, Schmid P, Tuerck D, Norcross RD,</br> Hoener MC, Spleiss O, Iglesias VA. A UGT2B10 splicing polymorphism common in</br> african populations may greatly increase drug exposure. J Pharmacol Exp Ther.</br> 2015 Feb;352(2):358-67. doi: 10.1124/jpet.114.220194. Epub 2014 Dec 12. PubMed</br> PMID: 25503386.</br>4: Thorn DA, Jing L, Qiu Y, Gancarz-Kausch AM, Galuska CM, Dietz DM, Zhang Y, Li </br> JX. Effects of the trace amine-associated receptor 1 agonist RO5263397 on</br> abuse-related effects of cocaine in rats. Neuropsychopharmacology. 2014</br> Sep;39(10):2309-16. doi: 10.1038/npp.2014.91. Epub 2014 Apr 18. PubMed PMID:</br> 24743376; PubMed Central PMCID: PMC4138753.</br>5: Thorn DA, Zhang C, Zhang Y, Li JX. The trace amine associated receptor 1</br> agonist RO5263397 attenuates the induction of cocaine behavioral sensitization in</br> rats. Neurosci Lett. 2014 Apr 30;566:67-71. doi: 10.1016/j.neulet.2014.02.024.</br> Epub 2014 Feb 21. PubMed PMID: 24561093; PubMed Central PMCID: PMC3991844.</br>6: Revel FG, Moreau JL, Pouzet B, Mory R, Bradaia A, Buchy D, Metzler V, Chaboz</br> S, Groebke Zbinden K, Galley G, Norcross RD, Tuerck D, Bruns A, Morairty SR,</br> Kilduff TS, Wallace TL, Risterucci C, Wettstein JG, Hoener MC. A new perspective </br> for schizophrenia: TAAR1 agonists reveal antipsychotic- and antidepressant-like</br> activity, improve cognition and control body weight. Mol Psychiatry. 2013</br> May;18(5):543-56. doi: 10.1038/mp.2012.57. Epub 2012 May 29. PubMed PMID:</br> 22641180.</br></br> |
