128196-01-0
中文名称
依他普仑
英文名称
Escitalopram
CAS
128196-01-0
分子式
C22H23FN2O5
MDL 编号
MFCD06407826
分子量
414.43
MOL 文件
128196-01-0.mol
更新日期
2024/04/27 20:13:22
128196-01-0 结构式
基本信息
中文别名
右旋西酞普兰依地普伦
1-(3-二甲基氨基丙基)-1-(4-氟苯基)-1,3-二氢异苯并呋喃-5-甲腈
依他普仑
英文别名
ESCITALOPRAM OXALATE(S)-(+)-CITALOPRAM OXALATE
(1R)-1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-3H-isobenzofuran-5-carbonitrile
1-(3-Dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile
Escitalopram
所属类别
生物化工：激动剂抑制剂物理化学性质
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Sealed in dry,2-8°C
溶解度溶于二甲基亚砜
酸度系数(pKa)9.57±0.28(Predicted)
形态粉末
常见问题列表
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. |