Agomelatine

产品说明书

Print
Chemical Structure| 138112-76-2 同义名 : S-20098
CAS号 : 138112-76-2
货号 : A643275
分子式 : C15H17NO2
纯度 : 98%
分子量 : 243.3
MDL号 : MFCD00916659
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • 5-HT2

  • 5-HT2
描述 Agomelatine behaves both as a potent agonist at melatonin MT1 and MT2 receptors and as a neutral antagonist at 5-HT2C receptors. Agomelatine dose-dependently inhibits the firing of cells in the SCN (the endogeneous master clock) in Syrian hamsters (ED50 = 0.91 mg/kg, i.p.)[3]. In CSDS (chronic social defeat stress) mice treated 3 weeks with 50 mg/kg/d agomelatine, the anxious-like phenotype was not reversed, but the treatment successfully prevented the cognitive impairments and hippocampal gene expression modifications[4].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
CHO cells Function assay 120 mins Displacement of [125I]iodomelatonin form human MT1 receptor expressed in CHO cells after 120 mins, Ki=0.1 nM 22301214
CHO-Galpha16 cells Function assay 20 mins Binding affinity to rat MT1 receptor expressed in CHO-Galpha16 cells assessed as Ca2+ mobilization after 20 mins by FLIPR assay, EC50=2.1 nM 21237644
HEK 293 Function assay Binding affinity for human Melatonin receptor type 1A stably transfected in human embryonic kidney cells (HEK 293) using 2-[125I]iodomelatonin as radioligand, Ki=6e-05 μM 12646022
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.11mL

0.82mL

0.41mL

20.55mL

4.11mL

2.06mL

41.10mL

8.22mL

4.11mL
参考文献

[1]Dagytė G, Crescente I, et al. Agomelatine reverses the decrease in hippocampal cell survival induced by chronic mild stress. Behav Brain Res. 2011 Mar 17;218(1):121-8.

[2]Zajecka J, Schatzberg A, et al. Efficacy and safety of agomelatine in the treatment of major depressive disorder: a multicenter, randomized, double-blind, placebo-controlled trial. J Clin Psychopharmacol. 2010 Apr;30(2):135-44.

[3]Guardiola-Lemaitre B, De Bodinat C, Delagrange P, Millan MJ, Munoz C, Mocaër E. Agomelatine: mechanism of action and pharmacological profile in relation to antidepressant properties. Br J Pharmacol. 2014 Aug;171(15):3604-19. doi: 10.1111/bph.12720. PMID: 24724693; PMCID: PMC4128060.

[4]Martin V, Allaïli N, Euvrard M, Marday T, Riffaud A, Franc B, Mocaër E, Gabriel C, Fossati P, Lehericy S, Lanfumey L. Effect of agomelatine on memory deficits and hippocampal gene expression induced by chronic social defeat stress in mice. Sci Rep. 2017 Apr 4;8:45907. doi: 10.1038/srep45907. PMID: 28374847; PMCID: PMC5379201.