1176316-99-6

1176316-99-6

中文名称1176316-99-6
中文同义词盐酸阿戈美拉汀
英文名称AgoMelatine (hydrochloride)
英文同义词AgoMelatine (hydrochloride);Agomelatine hydrochloride (S-20098 hydrochloride);S-20098 HYDROCHLORIDE;Agomelatine hydrochloride (S-20098 HCl)
CAS号1176316-99-6
分子式C15H18ClNO2
分子量279.76
EINECS号
相关类别
Mol文件1176316-99-6.mol
结构式1176316-99-6 结构式

1176316-99-6 性质

储存条件Store at -20°C
溶解度二甲基亚砜:≥100mg/mL(357.45mM)
形态粉末
颜色白色至米白色

1176316-99-6 用途与合成方法

Agomelatine hydrochloride (S-20098 hydrochloride) 是一种 MT1 和 MT2 受体的特异性激动剂,对 CHO-hMT1,HEK-hMT1,CHO-hMT2,HEK-hMT2 的 Ki 分别为 0.1,0.06,0.12 和 0.27 nM。Agomelatine hydrochloride 还是一种选择性的 5-HT2C 受体拮抗剂,在天然 (猪) 和克隆的人 5-HT2C 受体中 pKi 分别为 6.4 和 6.2。

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.

安全信息

MSDS信息

更新日期产品编号产品名称CAS号包装价格
2024/04/30HY-17038A1176316-99-6
Agomelatine hydrochloride
1176316-99-65mg460元
2024/04/30HY-17038A1176316-99-6
Agomelatine hydrochloride
1176316-99-610mM * 1mLin DMSO506元

1176316-99-6 上下游产品信息

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