依他普仑
| 中文名称 | 依他普仑 |
|---|---|
| 中文同义词 | 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;右旋西酞普兰;依地普伦;依地普仑 /草酸右旋西酞普兰;艾司西酞普兰;依他普仑;(+)-(S)-西酞普兰草酸盐;(+)-(S)-西酞普兰-D4草酸盐 |
| 英文名称 | Escitalopram |
| 英文同义词 | (1R)-1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-3H-isobenzofuran-5-carbonitrile;1-(3-Dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile;(S)-(+)-CITALOPRAM OXALATE;Escitalopram;(S)-CITALOPRAM S-(+)-1-3-(diMethyl-aMino) propyl-1-(p-fluorophenyl)-5-phthalancarbonitrile;EscitalopraM Oxalate INN;Seroplex;S-(+)-1-3-(dimethyl-amino) propyl-1-(p-fluorophenyl)-5-phthalancarbonitrile |
| CAS号 | 128196-01-0 |
| 分子式 | C20H21FN2O |
| 分子量 | 324.39 |
| EINECS号 | |
| 相关类别 | 医药原料;艾司西酞普兰原料药;艾司西酞普兰;小分子抑制剂;对照品;原料药;API;杂质对照品;中药对照品;神经系统药物 |
| Mol文件 | 128196-01-0.mol |
| 结构式 |  |
依他普仑 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 | 溶于二甲基亚砜 |
| 形态 | 粉末 |
| 酸度系数(pKa) | 9.57±0.28(Predicted) |
| CAS 数据库 | 128196-01-0(CAS DataBase Reference) |
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。
Ki: 0.89 nM (serotonin transporter), 10500 nM (DAT), 8150 nM (NET)
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. |
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