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1176316-99-6

中文名稱 1176316-99-6
英文名稱 AgoMelatine (hydrochloride)
CAS 1176316-99-6
分子式 C15H18ClNO2
分子量 279.76
MOL 文件 1176316-99-6.mol
1176316-99-6 結構式 1176316-99-6 結構式

基本信息

中文別名
鹽酸阿戈美拉汀
英文別名
S-20098 HYDROCHLORIDE
AgoMelatine (hydrochloride)
Agomelatine hydrochloride (S-20098 hydrochloride)
所屬類別
生物化工：激動劑抑制劑

物理化學性質

儲存條件-20°C儲存
溶解度DMSO: ≥ 100 mg/mL (357.45 mM)
形態(tài)粉末
顏色White to off-white
鹽酸阿戈美拉汀價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2025/02/05HY-17038A1176316-99-6
Agomelatine hydrochloride		1176316-99-65mg460元
2025/02/05HY-17038A1176316-99-6
Agomelatine hydrochloride		1176316-99-610mM * 1mLin DMSO506元
2025/02/05HY-17038A1176316-99-6
Agomelatine hydrochloride		1176316-99-610mg714元

常見問題列表

生物活性
Agomelatine hydrochloride (S-20098 hydrochloride) 是一種 MT1 和 MT2 受體的特異性激動劑，對 CHO-hMT1，HEK-hMT1，CHO-hMT2，HEK-hMT2 的 Ki 分別為 0.1，0.06，0.12 和 0.27 nM。Agomelatine hydrochloride 還是一種選擇性的 5-HT2C 受體拮抗劑，在天然 (豬) 和克隆的人 5-HT2C 受體中 pKi 分別為 6.4 和 6.2。
靶點

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)

體外研究

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.

體內(nèi)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.
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