同义名 :	依他普仑 ;(S)-(+)-Citalopram; (S)-Citalopram; Seroplex
	CAS号 :	128196-01-0
	货号 :	A247040
	分子式 :	C20H21FN2O
	纯度 :	98%
	分子量 :	324.39
	MDL号 :	MFCD09817397
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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].

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 <<

实验方案
	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

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.