Agomelatine 阿戈美拉汀
货号：
IA0120
品牌：
Jinpan
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产品简介
| EC | EINECS 629-727-7 |
| MDL | MFCD00916659 |
| 别名 | N-[2-(7-甲氧基-1-萘基)乙基]乙酰胺 |
| CAS | 138112-76-2 |
| 分子式 | C15H17NO2 |
| 分子量 | 243.3 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | Agomelatine (S20098; AGO-178; S-20098; AGO178; Valdoxan, Melitor, Thymanax) is a potent and specific agonist of MT1 and MT2 receptors with anti-depressive activity. It activates the isoforms of MT receptors such as CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2 with Kis of 0.1, 0.06, 0.12, and 0.27 nM, respectively. It is a unique antidepressant and is developed for treatment of major depressive disorder (MDD). It shows low affinities to cloned human 5-HT2A and 5-HT1A. In the in vivo studies, agomelatine causes increase of dopamine and noradrenaline levels via blocking the inhibitory input of 5-HT2C.[1] |
| In Vitro | 在慢性应激电击的小鼠的海马中，Agomelatine完全正常化压力影响的细胞生存并部分逆转降低的doublecortin表达。[1] |
| In Vivo | 转基因小鼠中，Agomelatine有效扭转了强迫游泳试验，以及在高架十字迷宫的行为改变。Agomelatine也显著加快了温度和活性的昼夜周期的调整，接下来是诱导的内容相移。[2] |
| SMILES | CC(NCCC1=C2C=C(OC)C=CC2=CC=C1)=O |
| 靶点 | 5-HT Receptor |
| 数据来源文献 | [1]. Behav Brain Res. 2011 Mar 17;218(1):121-8 [2]. Prog Neuropsychopharmacol Biol Psychiatry. 2005 Jul;29(6):908-16. |
| 规格 | 10mg 10mM*1mL (in DMSO) 50mg |
对 5-HT2C 受体具有拮抗作用，因而是一种去甲肾上腺素-多巴胺抑制解除剂（NDDI）。