| Description | RO5166017 is an orally active, potent and selective trace amine-associated receptor 1 (TAAR1) agonist for the study of conditioned taste aversion frontal nerve disorders. |
| In vitro | RO5166017 对稳定表达在HEK293细胞中的小鼠/大鼠/食蟹猴/人类TAAR1展现出高亲和力和强大的功能活性，并相对于其他目标展示出高选择性[2]。 |
| In vivo | RO5166017抑制应激诱导的高体温并阻断可卡因处理的和多巴胺转运体敲除小鼠的多巴胺依赖性高活动性，以及NMDA拮抗剂引起的过度活跃[2]。口服剂量为0.01-1 mg/kg时，RO5166017剂量依赖性地预防NMRI小鼠的应激诱导高体温。在0.1-0.3 mg/kg的剂量下，RO5166017表现出TAAR1介导的类抗焦虑属性[2]。RO5166017预防可卡因诱发的高活动性并抑制WT小鼠的可卡因诱发的刻板行为，类似于奥氮平的效果，但在Taar1小鼠中这一效果消失[1]。RO5166017通过激活TAAR1在INS1E细胞和人类胰岛中增加葡萄糖依赖的胰岛素分泌，并在小鼠中提升血浆中肽YY (PYY) 和类胰高血糖素1 (GLP-1) 的水平[1]。长期治疗饮食诱导的肥胖（DIO）小鼠，RO5166017减少食物摄入和体重[1]。 |
| Synonyms | RO 5166017, RO-5166017 |
| molecular weight | 219.28 |
| Molecular formula | C12H17N3O |
| CAS | 1048346-74-2 |
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 20 mg/mL (91.21 mM), Sonication is recommended. |
| References | 1. Justin N Siemian, et al. Trace amine-associated receptor 1 agonists RO5263397 and RO5166017 attenuate quinpirole-induced yawning but not hypothermia in rats. Behav Pharmacol. 2017 Oct;28(7):590-593. 2. Revel FG,et al. TAAR1 activation modulates monoaminergic neurotransmission, preventing hyperdopaminergic and hypoglutamatergic activity. Proc Natl Acad Sci U S A. 2011 May 17;108(20):8485-90. 3. Cichero E, Espinoza S, Franchini S, Guariento S, Brasili L, Gainetdinov RR, Fossa P. Further insights into the pharmacology of the human trace amine-associated receptors: discovery of novel ligands for TAAR1 by a virtual screening approach. Chem Biol Drug Des. 2014 Dec;84(6):712-20. doi: 10.1111/cbdd.12367. Epub 2014 Jun 30. PubMed PMID: 24894156. 4. Leo D, Mus L, Espinoza S, Hoener MC, Sotnikova TD, Gainetdinov RR. Taar1-mediated modulation of presynaptic dopaminergic neurotransmission: role of D2 dopamine autoreceptors. Neuropharmacology. 2014 Jun;81:283-91. doi: 10.1016/j.neuropharm.2014.02.007. Epub 2014 Feb 22. PubMed PMID: 24565640. |