Escitalopram-d6 oxalate(Synonyms: 依他普仑草酸盐 d6 (草酸盐))

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Escitalopram-d6 oxalate (Synonyms: 依他普仑草酸盐 d6 (草酸盐))

Escitalopram-d6 oxalate 是 Escitalopram oxalate 的氘代物。Escitalopram ((S)-Citalopram) oxalate 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 oxalate 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 oxalate 是研究抑郁症的抗抑郁药。

Escitalopram-d6 oxalate(Synonyms: 依他普仑草酸盐 d6 (草酸盐))

Escitalopram-d6 oxalate Chemical Structure

CAS No. : 1217733-09-9

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生物活性

Escitalopram-d6 oxalate is the deuterium labeled Escitalopram oxalate. Escitalopram ((S)-Citalopram) oxalate, the S-enantiomer of racemic Citalopram, is a selective serotonin reuptake inhibitor (SSRI) with a Ki of 0.89 nM. Escitalopram oxalate has ∼30 fold higher binding affinity than its R(-)-enantiomer and shows selectivity over both dopamine transporter (DAT) and norepinephrine transporter (NET). Escitalopram oxalate is an antidepressant for the research of major depression[1][2].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

420.46

Formula

C22H17D6FN2O5

CAS 号

1217733-09-9

中文名称

依他普仑草酸盐 d6 (草酸盐)

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. 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.

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

    [4]. 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.

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

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