依他普仑

生物活性靶点体内研究依他普仑试剂级价格

依他普仑

CAS号:128196-01-0
英文名:Escitalopram
中文名:依他普仑
CBNumber:CB2712918
分子式:C20H21FN2O
分子量:324.39
MOL File:128196-01-0.mol

依他普仑化学性质

比旋光度 :D +12.33° (c = 1 in methanol)
沸点 :428.3±45.0 °C(Predicted)
密度 :1.18±0.1 g/cm3(Predicted)
储存条件 :2-8°C
溶解度 :Soluble in DMSO
形态 :Powder
酸度系数(pKa) :9.57±0.28(Predicted)
颜色 :Off-white to light yellow
CAS 数据库 :128196-01-0(CAS DataBase Reference)

安全信息

毒害物质数据 :128196-01-0(Hazardous Substances Data)

依他普仑性质、用途与生产工艺

生物活性 Escitalopram ((S)-Citalopram) 是外消旋 Citalopram 的 S-对映体，是一种选择性 5-羟色胺再摄取抑制剂 (SSRI)，Ki 为 0.89 nM，比 R(-)-enantiomer 结合亲和力高 30 倍。Escitalopram 对多巴胺转运体 (DAT) 和去甲肾上腺素转运体 (NET) 均有选择性。Escitalopram 是研究抑郁症的抗抑郁药。
靶点

Ki: 0.89 nM (serotonin transporter), 10500 nM (DAT), 8150 nM (NET)

体内研究

Escitalopram (10 mg/kg; i.p.; daily for 28 days) ameliorates cognitive impairments and selectively attenuates phosphorylated tau accumulation in stressed rats.
Chronic administration of Escitalopram (daily; drinking water for a total of 4 months) significantly reduces plaque load by 28% and 34% at 2.5 and 5 mg/d, respectively .

Animal Model:	Male Sprague-Dawley rats
Dosage:	10 mg/kg
Administration:	I.p.; daily for 28 days
Result:	Could selectively decrease phosphorylated tau accumulation in the hippocampus of stressed rats and could distinctly alleviate the hyperactivity of the HPA axis in both depressive and resistant rats.

Animal Model:	APP-PS1 hemizygous female mice (4 months of age)
Dosage:	2.5-5 mg/kg
Administration:	Daily; drinking water for a total of 4 months
Result:	At both doses significantly reduced plaque burden within the brains of these mice compared to littermate controls that drank only water. Hippocampal plaque load was significantly reduced by 28.7% and 34.4 % for ESC 2.5 mg/day and 5 mg/day, respectively.