Citalopram hydrobromide

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CAS NO:

59729-32-7

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

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。

生物活性

Citalopram hydrobromide is aselective serotonin reuptake inhibitor (SSRI). Citalopram hydrobromide inhibits 5-HT uptake into synaptosomes with anIC₅₀of 1.8 nM. Citalopram hydrobromideinhibits the 5-HT uptake in rabbit blood platelets with an IC₅₀of 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].

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].

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

性状

Solid

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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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本网站选购。