128196-01-0
中文名稱
依他普侖
英文名稱
Escitalopram
CAS
128196-01-0
分子式
C22H23FN2O5
MDL 編號(hào)
MFCD06407826
分子量
414.43
MOL 文件
128196-01-0.mol
更新日期
2024/10/23 16:26:33
128196-01-0 結(jié)構(gòu)式
基本信息
中文別名
右旋西酞普蘭依地普倫
1-(3-二甲基氨基丙基)-1-(4-氟苯基)-1,3-二氫異苯并呋喃-5-甲腈
依他普侖
英文別名
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
所屬類別
生物化工：激動(dòng)劑抑制劑物理化學(xué)性質(zhì)
比旋光度D +12.33° (c = 1 in methanol)
沸點(diǎn)428.3±45.0 °C(Predicted)
密度1.18±0.1 g/cm3(Predicted)
儲(chǔ)存條件Sealed in dry,2-8°C
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)9.57±0.28(Predicted)
形態(tài)粉末
顏色Off-white to light yellow
CAS 數(shù)據(jù)庫(kù)128196-01-0(CAS DataBase Reference)
常見問題列表
生物活性
Escitalopram ((S)-Citalopram) 是外消旋 Citalopram 的 S-對(duì)映體，是一種選擇性 5-羥色胺再攝取抑制劑 (SSRI)，Ki 為 0.89 nM，比 R(-)-enantiomer 結(jié)合親和力高 30 倍。Escitalopram 對(duì)多巴胺轉(zhuǎn)運(yùn)體 (DAT) 和去甲腎上腺素轉(zhuǎn)運(yùn)體 (NET) 均有選擇性。Escitalopram 是研究抑郁癥的抗抑郁藥。靶點(diǎn)
Ki: 0.89 nM (serotonin transporter), 10500 nM (DAT), 8150 nM (NET)
體內(nèi)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. |