1176316-99-6

生物活性靶点体外研究体内研究 1176316-99-6 试剂级价格

1176316-99-6

CAS号:1176316-99-6
英文名:AgoMelatine (hydrochloride)
中文名:1176316-99-6
CBNumber:CB42677042
分子式:C15H18ClNO2
分子量:279.76
MOL File:1176316-99-6.mol

1176316-99-6化学性质

储存条件 :Store at -20°C
溶解度 :DMSO: ≥ 100 mg/mL (357.45 mM)
形态 :Powder
颜色 :White to off-white

1176316-99-6性质、用途与生产工艺

生物活性 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。

靶点

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)

体外研究

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.

体内研究

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.