Citalopram hydrobromide(Synonyms: 氢溴酸西酞普兰; (±)-Citalopram hydrobromide; Lu 10-171)

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Citalopram hydrobromide (Synonyms: 氢溴酸西酞普兰; (±)-Citalopram hydrobromide; Lu 10-171) 纯度: 99.66%

Citalopram hydrobromide 是一种选择性血清素再摄取抑制剂 (SSRI)。 Citalopram hydrobromide 抑制 5-HT 摄取进入突触体,IC50 为 1.8 nM。 Citalopram hydrobromide 抑制兔血小板中 5-HT 的摄取,IC50 为 14 nM。具有抗抑郁作用。

Citalopram hydrobromide(Synonyms: 氢溴酸西酞普兰; (±)-Citalopram hydrobromide;  Lu 10-171)

Citalopram hydrobromide Chemical Structure

CAS No. : 59729-32-7

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生物活性

Citalopram hydrobromide is a selective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with an IC50 of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC50 of 14 nM. Antidepressant effect[1].

体外研究
(In Vitro)

Citalopram(25-150 μM) shows a concentration-dependent cytotoxicity on the viability of rat B104, human SH-SY5Y, IMR32 and Kelly neuroblastoma cell lines and human primary Schwann cells (HSC)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Rat B104, human SH-SY5Y, IMR32 and Kelly neuroblastoma cells
Concentration: 50, 100, 125, 150 μM for B104 cells
25, 50, 100, 125 μM for SH-SY5Y cells
25, 50, 100, 125, 150 μM for Kelly cells
25, 50, 100, 125 μM for IMR32 cells
50, 100, 125, 150 μM for HSCs
Incubation Time: 24 h ours
Result: Significantly decreased B104 cell viability, 61%, 33% and 11% at respectively 100, 125 and 150 μM in B104 cell line.
Drastically decreased SH-SY5Y cell viability, 17%, 1% at respectively 100 and 125 μM in SH-SY5Y cell line.
Significantly decreased Kelly cell viability, 64%, 9% and 0% at respectively 100, 125 and 150 μM in Kelly cell line.
Drastically decreased IMR32 cell viability, 36%, 1% and 0% at respectively 50, 100 and 125 μM in IMR32 cell line.

体内研究
(In Vivo)

Acute administration of Citalopram (1-10 mg/kg, i.p. 1 h before an elevated plus-maze test) to Spontaneously Hypertensive rats (SHRs), Lewis (LEW) rats, and Wistar-Kyoto (WKY) rats, i.e., rat strains differing for their emotionality, promotes anxiety, and/or hypoactivity, except in WKY rats. In the three strains, such a pretreatment increased central 5-HT levels and/or decreased 5-hydroxyindoleacetic acid levels[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male rats from the SHR, LEW, and WKY strains, aged 6–8 weeks[3]
Dosage: 1, 3.3, or 10 mg/kg
Administration: Injected i.p.
Result: Increased significantly 5-HT in SHRs and WKY rats, and decreased 5-HIAA in all strains, in either a dose-dependent (LEW and WKY rats) or a dose-independent (SHRs) manner.

Clinical Trial

分子量

405.30

Formula

C20H22BrFN2O

CAS 号

59729-32-7

中文名称

氢溴酸西酞普兰

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 38 mg/mL (93.76 mM)

H2O : 10 mg/mL (24.67 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.4673 mL 12.3365 mL 24.6731 mL
5 mM 0.4935 mL 2.4673 mL 4.9346 mL
10 mM 0.2467 mL 1.2337 mL 2.4673 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 110 mg/mL (271.40 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.17 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.17 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. J Hyttel. Citalopram–pharmacological profile of a specific serotonin uptake inhibitor with antidepressant activity. Prog Neuropsychopharmacol Biol Psychiatry. 1982;6(3):277-95.

    [2]. Laurent Sakka, et al. Assessment of citalopram and escitalopram on neuroblastoma cell lines. Cell toxicity and gene modulation. Oncotarget. 2017 Jun 27;8(26):42789-42807.

    [3]. F Pollier, et al. Serotonin reuptake inhibition by citalopram in rat strains differing for their emotionality. Neuropsychopharmacology. 2000 Jan;22(1):64-76.

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