產品屬性：
產品名稱 | RO5166017 |
規格 | 5mg、10mg、25mg |
貨號 | EY-01Y17973 |
Cas No.: 1048346-74-2
別名: N/A
化學名: N/A
分子式: C12H17N3O
分子量: 219.3
溶解度: DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:2): 0.33 mg/ml,DMSO: 10 mg/ml,Ethanol: 10 mg/ml
儲存條件: -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
RO5166017 is an agonist of trace amine-associated receptor 1 (TAAR1).1 It binds to TAAR1 (Kis = 31, 24, 1.9, and 2.7 nM in HEK293 cells expressing the recombinant human, cynomolgus monkey, mouse, or rat receptor, respectively) and is greater than 15-fold selective for TAAR1 over a panel of 123 receptors, ion channels, and transporters at 10 μM. RO5166017 induces cAMP production in HEK293 cells expressing the recombinant human, cynomolgus monkey, mouse, or rat TAAR1 (EC50s = 55, 97, 3.3, and 14 nM, respectively). It reduces the frequency of neuronal firing in mouse ventral tegmental area (VTA) and dorsal raphe nucleus (DRN) slices (IC50s = 1.73 and 2.99 nM, respectively), which endogenously express high levels of dopaminergic and serotonergic neurons, respectively. RO5166017 (0.3 mg/kg) inhibits stress-induced hyperthermia, indicating anxiolytic-like activity, as well as reduces cocaine-induced hyperlocomotion, in mice. It also impairs expression, but not reconsolidation, of cocaine-induced place preference in rats.21.Revel, F.G., Moreau, J.-L., Gainetdinov, R.R., et al.TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activityProc. Natl. Acad. Sci. USA108(20)8485-8490(2011)
2.Liu, J.-F., Thorn, D.A., Zhang, Y., et al.Effects of trace amine-associated receptor 1 agonists on the expression, reconsolidation, and extinction of cocaine reward memoryInt. J. Neuropsychopharmacol.19(7)pyw009(2016)
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