Escitalopram (Synonyms:艾司西酞普兰; (S)-Citalopram; (S)-(+)-Citalopram)
目录号 : KCM10920 CAS No. : 128196-01-0 纯度 : ≥98%
Escitalopram is a selective serotonin (5-HT) reuptake inhibitor (SSRI) and the (S) isomer of citalopram and (R)-citalopram. It selectively binds to SERT (K = 0.89 nM) over the norepinephrine and dopamine transporters (Ks = >10,000 and 8,150 nM, respectively) and inhibits 5-HT reuptake in rat brain synaptosomes (IC = 2.1 nM). Escitalopram reduces immobility in the forced swim test in mice (ED = 12 mg/kg), indicating anti-depressant-like activity, and increases exploratory behavior in the black-and-white box test in mice with a minimal effective dose (MED) of 0.49 mg/kg, indicating anxiolytic-like activity. Escitalopram (20 µM) prevents acid sphingomyelinase activation and subsequent ceramide release induced by infection with replication-deficient vesicular stomatitis virus pseudoviral particles (pp-VSV) presenting the severe acute respiratory coronavirus 2 (SARS-CoV-2) spike protein in Vero cells, an effect that can be overcome with exogenous application of C16 ceramide . Formulations containing escitalopram have been used in the treatment of major depressive disorder (MDD) and generalized anxiety disorder (GAD).
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生物活性

Escitalopram, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram is an antidepressant for the research of major depression[1].

IC50&Target

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.
 
分子式
C20H21FN2O
分子量
324.39
CAS号
128196-01-0
中文名称
依他普仑;艾司西酞普兰
储存方式
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶解性数据

Room temperature in continental US; may vary elsewhere.

[1]. Zhang, P., et al., Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbon itrile) analogues at monoamine transporters. J Med Chem, 2010. 53(16): p. 6112-21.

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