产品
编 号:F144859
分子式:C15H17NO2
分子量:243.3
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
184
In-stock
5mg
368
In-stock
10mg
572
In-stock
50mg
1828
In-stock
100mg
2772
In-stock
结构图
联系客服
产品详情
生物活性:
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

体内研究:
Agomelatine (25、50 或 75 mg/kg;ip) 在 Strychnine (75 mg/kg,ip) 或 Pilocarpine (400 mg/kg,ip) 诱导的小鼠癫痫发作模型中具有抗氧化活性。与对照组相比,Agomelatine 剂量对戊四唑 (PTZ) 或印防己毒素 (PTX) 诱导的癫痫发作模型产生的氧化应激参数没有任何抗氧化作用。Animal Model:Female Swiss mice (20-30 g) were administered PTZ (85 mg/kg, i.p.), PTX (7 mg/kg, i.p.), strychnine (75 mg/kg, i.p.), Pilocarpine (400 mg/kg, i.p.), respectively.
Dosage:25, 50, or 75 mg/kg
Administration:Administered intraperitoneally (i.p.)
Result:All dosages showed a significant decrease in thiobarbituric acid reactive substances (TBARS) levels and nitrite content in all brain areas when compared to controls in the Pilocarpine induced seizure model.All dosages decreased TBARS levels in all brain areas, and at low doses (25 or 50 mg/kg) decreased nitrite contents, but only at 25 or 50 mg/kg showed a significant increase in catalase activity in three brain areas when compared to controls in the Strychnine-induced seizure model.Did not have any antioxidant effects on parameters of oxidative stress produced by PTX- or PTZ-induced seizure models when compared to controls.

体外研究:
Agomelatine (S 20098) 作为 MT1 和 MT2 受体的完全激动剂,对 CHO hMT1、CHO-hMT2 (hMT1 和 hMT2 受体在 CHO 中表达) 的 EC50 为 1.6±0.4,0.10±0.04 nM或 HEK 细胞膜)。 Agomelatine (S20098) 也与 h5-HT2B 受体 (6.6) 相互作用,而 Agomelatine 对天然 (大鼠)/克隆的人类 5 表现出低亲和力-HT2A (Agomelatine 相关抗体:
产品资料