1176316-99-6
1176316-99-6 用途与合成方法
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5-HT 2C Receptor 6.4 (pKi, native porcine) |
5-HT 2C Receptor 6.2 (pKi, human) |
hMT1 0.1 (Ki, CHO Cells) |
hMT1 0.06 (Ki, HEK Cells) |
hMT2 0.12 (Ki, CHO Cells) |
hMT2 0.27 (Ki, HEK Cells) |
Agomelatine (S 20098) acts as a full agonist of MT1 and MT2 receptors with EC
50
s of 1.6±0.4, 0.10±0.04 nM for CHO hMT1 CHO-hMT2 (hΜΤ1 and hΜΤ2 receptors expressed in CHO or HEK cell membranes).
Agomelatine (S20098) also interacts with h5-HT2B receptors (6.6), whereas it shows low affinity at native (rat)/cloned, human 5-HT2A (<5.0/5.3) and 5-HT1A (<5.0/5.2) receptors, and negligible (<5.0) affinity for other 5-HT receptors.
Agomelatine (25, 50, or 75 mg/kg; i.p.) has antioxidant activity in Strychnine (75 mg/kg, i.p.) or Pilocarpine (400 mg/kg, i.p.) induced seizure models in mice. Agomelatine dose not have any antioxidant effects on parameters of oxidative stress produced by Pentylenetetrazole (PTZ) or Picrotoxin (PTX) induced seizure models when compared to controls.
| 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. |
1176316-99-6 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-01-25 | HY-17038A | 1176316-99-6 | 1176316-99-6 | 5mg | 460 |
| 2024-01-25 | HY-17038A | 1176316-99-6 | 1176316-99-6 | 10mM * 1mLin DMSO | 506 |
