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艾司西酞普兰 /Escitalopram {[allProObj[0].p_purity_real_show]}

货号:A247040 同义名: 依他普仑 / (S)-(+)-Citalopram;(S)-Citalopram

Escitalopram is a selective serotonin reuptake inhibitor (SSRI) with Ki of 0.89 nM.

Escitalopram 化学结构 CAS号:128196-01-0
Escitalopram 化学结构
CAS号:128196-01-0
Escitalopram 3D分子结构
CAS号:128196-01-0
Escitalopram 化学结构 CAS号:128196-01-0
Escitalopram 3D分子结构 CAS号:128196-01-0
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Escitalopram 纯度/质量文件 产品仅供科研

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Escitalopram 生物活性

描述 The serotonergic system in the brain modulates many types of behavioural and physiological processes. An example of this modulatory function is seen with the selective serotonin reuptake inhibitors (SSRIs) which enhance serotonin transmission and influence mood, anxiety states, aggression, feeding and sexual behaviour[3]. SSRIs are widely used antidepressants characterized by less-frequent adverse effects compared with classical anti-depressive agents. On the other hand, SSRI can cause hemorrhagic events more due to impaired platelet aggregation induced by a depletion of serotonin in the peripheral platelet[4].Escitalopram ((S)-Citalopram), the S-enantiomer of racemic Citalopram, is a 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[5].Escitalopram (10 mg/kg; i.p.; daily for 28 days) ameliorates cognitive impairments and selectively attenuates phosphorylated tau accumulation in stressed rats[6].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[7].

Escitalopram 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00707863 Major Depression Phase 4 Completed - United States, Indiana ... 展开 >> Indiana University Adult Psychiatric Clinic Indianapolis, Indiana, United States, 46202 收起 <<
NCT00707863 - Completed - -
NCT00232700 Major Depressive Disorder Not Applicable Completed - Germany ... 展开 >> Department of Psychiatry, Charité - Universitaetsmedizin Berlin, Campus Benjamin Franklin Berlin, Germany, 14050 收起 <<

Escitalopram 参考文献

[1]Pastoor D, Gobburu J. Clinical pharmacology review of escitalopram for the treatment of depression. Expert Opin Drug Metab Toxicol. 2014 Jan;10(1):121-8.

[2]Zhang P, Cyriac G, et al. Structure-activity relationships for a novel series of citalopram (1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile) analogues at monoamine transporters. J Med Chem. 2010 Aug 26;53(16):6112-21.

[3] B Olivier,R van Oorschot, M D Waldinger. Serotonin, serotonergic receptors, selective serotonin reuptake inhibitors and sexual behaviour. Int Clin Psychopharmacol.1998 Jul;13 Suppl 6:S9-14.

[4]Takatsugu Yamamoto, Koichiro Abe, Yasushi Kuyama. Selective serotonin reuptake inhibitor and gastrointestinal hemorrhage. Nihon Rinsho. 2013 Apr;71(4):751-6.

[5]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.

[6]Wu C , et al. Escitalopram alleviates stress-induced Alzheimer's disease-like tau pathologies and cognitive deficits by reducing hypothalamic-pituitary-adrenal axis reactivity and insulin/GSK-3β signal pathway activity. Neurobiol Aging. 2018;67:137-147.

[7]Cirrito JR, et al. Effect of escitalopram on Aβ levels and plaque load in an Alzheimer mouse model. Neurology. 2020;95(19):e2666-e2674.

Escitalopram 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.08mL

0.62mL

0.31mL

15.41mL

3.08mL

1.54mL

30.83mL

6.17mL

3.08mL

Escitalopram 技术信息

CAS号128196-01-0
分子式C20H21FN2O
分子量 324.392
别名 依他普仑 ;(S)-(+)-Citalopram;(S)-Citalopram;Seroplex
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 105 mg/mL(323.68 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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