| CAS |
138112-76-2 |
| Chinese Name |
阿戈美拉汀 |
| English Name |
Agomelatine |
| Synonyms |
;N-[2-(7-甲氧基-1-萘基)乙基]乙酰胺;阿戈美拉汀(I型);阿戈美拉汀;N-[2-(7-甲氧基萘-1-基)乙基]乙酰胺; |
| Molecular Formula |
C15H17NO2 |
| Molecular Weight |
243.3 |
| Solubility |
Soluble in DMSO ≥10mg/mL |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 629-727-7 |
| MDL |
MFCD00916659 |
| SMILES |
CC(NCCC1=C2C=C(OC)C=CC2=CC=C1)=O |
| InChIKey |
YJYPHIXNFHFHND-UHFFFAOYSA-N |
| InChI |
InChI=1S/C15H17NO2/c1-11(17)16-9-8-13-5-3-4-12-6-7-14(18-2)10-15(12)13/h3-7,10H,8-9H2,1-2H3,(H,16,17) |
| PubChem CID |
82148 |
| Target Point |
Melatonin Receptor; 5-HT Receptor |
| Passage |
GPCR/G Protein; Neuronal Signaling |
| Background |
Agomelatine is a specific agonist for the MT1 and MT2 receptors. Agomelatine is also a selective 5-HT2C receptor antagonist. |
| Biological Activity |
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] |
| Data Literature Source |
[1]. Behav Brain Res. 2011 Mar 17;218(1):121-8
[2]. Prog Neuropsychopharmacol Biol Psychiatry. 2005 Jul;29(6):908-16. |
| Unit |
Bottle |
| Specification |
10mg 10mM*1mL in DMSO 50mg |
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