| 名称 | Agomelatine hydrochloride |
| 描述 | Agomelatine hydrochloride (S-20098 hydrochloride) is a specific MT1 and MT2 receptor agonist with Ki values of 0.1 nM for CHO-hMT1, 0.06 nM for HEK-hMT1, 0.12 nM for CHO-hMT2, and 0.27 nM for HEK-hMT2, respectively [1]. Additionally, Agomelatine hydrochloride is a selective antagonist of the 5-HT2C receptor with pKi values of 6.4 and 6.2 for native (porcine) and cloned human 5-HT2C receptors, respectively [2]. |
| 体外活性 | Agomelatine (S 20098) functions as a full agonist for the MT1 and MT2 receptors, exhibiting EC50 values of 1.6±0.4 and 0.10±0.04 nM, respectively, when expressed in CHO or HEK cell membranes. Additionally, Agomelatine interacts with h5-HT2B receptors, displaying a marked preference (6.6). However, it demonstrates low affinity for both native and cloned human 5-HT2A receptors, with values just below 5.0/5.3, and similarly low affinity for 5-HT1A receptors (below 5.0/5.2), while exhibiting negligible affinity for other 5-HT receptors. |
| 体内活性 | Agomelatine (25, 50, or 75 mg/kg; i.p.) exhibits antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice, but does not affect oxidative stress parameters in Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models compared to controls[3]. |
| 存储条件 | Shipping with blue ice. |
| 溶解度 | H2O : 0.1 mg/mL (insoluble)
DMSO : 90 mg/mL (321.7 mM)
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| 关键字 | S-20098 Hydrochloride | Agomelatine Hydrochloride | S 20098 Hydrochloride | S20098 Hydrochloride |
| 相关产品 | 8-M-PDOT | Ramelteon | ACH-000143 | glycine | 4-P-PDOT | Tasimelteon | Piromelatine | S26131 | Luzindole |
| 相关库 | FDA上市及药典收录分子库 | 神经退行性疾病化合物库 | 经典已知活性库 | 抗抑郁症化合物库 | 神经信号分子库 | EMA 上市药物库 | 药物功能重定位化合物库 | 抑制剂库 | 临床期小分子药物库 | 已知活性化合物库 |
United States
