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Citalopram HBr/氢溴酸西肽普兰 {[allProObj[0].p_purity_real_show]}

货号:A300817 同义名: 氢溴酸西酞普兰 / Lu 10-171; (±)-Citalopram hydrobromide

Citalopram HBr是一种高选择性且有效的 5-HT 再摄取抑制剂,对去甲肾上腺素或多巴胺的再摄取没有影响。

Citalopram HBr/氢溴酸西肽普兰 化学结构 CAS号:59729-32-7
Citalopram HBr/氢溴酸西肽普兰 化学结构
CAS号:59729-32-7
Citalopram HBr/氢溴酸西肽普兰 3D分子结构
CAS号:59729-32-7
Citalopram HBr/氢溴酸西肽普兰 化学结构 CAS号:59729-32-7
Citalopram HBr/氢溴酸西肽普兰 3D分子结构 CAS号:59729-32-7
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Citalopram HBr/氢溴酸西肽普兰 纯度/质量文件 产品仅供科研

货号:A300817 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

98%
Venlafaxine 99%
Fluvoxamine maleate 99%
Iloperidone 99%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 97%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 99%
Fluoxetine HCl 99.5%
Paroxetine HCl AChR 99%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

95%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

99%
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (human), Ki: 6.8 nM

5-HT2 (bovine), Ki: 6.6 nM

98%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 99%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pKi: 9.5

5-HT2B, pIC50: 10.4

99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

98%
Tropisetron 99%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron HCl dihydrate 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron HCl ++++

5-HT3, IC50: 0.33 nM

99%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

95%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Citalopram HBr/氢溴酸西肽普兰 生物活性

靶点
  • 5-HT

    serotonin reuptake, IC50:1.8 nM

描述 Citalopram hydrobromide, a selective serotonin reuptake inhibitor (SSRI), blocks the uptake of 5-HT into synaptosomes with an IC50 of 1.8 nM and into rabbit blood platelets with an IC50 of 14 nM, displaying antidepressant effects[1].
体内研究

Acute administration of Citalopram (1-10 mg/kg, i.p., 1 h before an elevated plus-maze test) to different rat strains (Spontaneously Hypertensive rats, Lewis rats, and Wistar-Kyoto rats), which vary in their emotional responses, generally induces anxiety and/or hypoactivity, except in Wistar-Kyoto rats. This pretreatment also alters central serotonin levels and/or reduces 5-hydroxyindoleacetic acid levels in these strains[3].

体外研究

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

Citalopram HBr/氢溴酸西肽普兰 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
APP/PS1 mice Transgenic AD mouse model Intraperitoneal injection 2.5, 5, 10, 20 mg/kg 24 hours after single dose Citalopram decreased brain ISF Aβ concentrations in a dose-dependent manner, with 10 mg/kg being the most effective dose. Sci Transl Med. 2014 May 14;6(236):236re4
Mice APP/PS1 transgenic mouse model Intraperitoneal injection 10 mg/kg Single dose To investigate the effect of Citalopram on brain interstitial fluid Aβ levels, results showed a significant reduction in Aβ levels 16 hours after a single dose. Mol Neurodegener. 2016 Jun 18;11(1):45
Mice Wild-type and Eif4e ki/ki mice Intraperitoneal injection 10 mg/kg 3 doses Investigated the effect of Citalopram on eIF4E phosphorylation, showing no change in eIF4E phosphorylation levels Nat Commun. 2018 Jun 25;9(1):2459
AppNL-G-F/NL-G-F knock-in mice Alzheimer's disease model Dietary administration 10 mg/kg/day Once daily for 8 weeks To evaluate the effects of polypharmacy on Alzheimer's disease pathology and behavior. Results showed that the combination therapy (including citalopram) improved memory and reduced amyloid plaque burden in male mice, with negligible effects in female mice. Alzheimers Dement. 2025 Mar;21(3):e70081
Mice Chronic restraint stress model Intraperitoneal injection 10 mg/kg/d Once daily for 21 days Citalopram partially reversed the depression- and anxiety-like behavioral changes induced by chronic stress, manifesting as decreased immobility time in the FST and increased sucrose consumption in the SPT. Gut Microbes. 2021 Jan-Dec;13(1):1-16
C57BL/6 mice HCC subcutaneous xenograft model Intraperitoneal injection 10 mg/kg Once every 4 days for 20 days To evaluate the effect of escitalopram on HCC tumor growth and its synergistic effect with anti-PD1 immunotherapy. Results showed that escitalopram significantly inhibited tumor growth and enhanced the sensitivity of anti-PD1 immunotherapy. J Immunother Cancer. 2022 Dec;10(12):e005655.
129S1/SVImJ mice Forced swim test (FST), tail suspension test (TST), learned helplessness (LH) paradigm, female urine sniffing test (FUST) Intracerebroventricular infusion 20 µM 6 µl per day for 14 days Citalopram and BI-11A7 significantly reduced immobility time in the FST and TST, attenuated escape latencies in the LH paradigm, and significantly improved duration of female urine sniffing in helpless mice in the FUST. Mol Psychiatry. 2012 Jul;17(8):770-80
Mice Machado-Joseph disease model Oral 8 and 13 mg/kg/day From 5 weeks of age until 34 weeks of age Citalopram significantly reduced ataxin 3 neuronal inclusions and astrogliosis, rescued diminished body weight and strikingly ameliorated motor symptoms. Brain. 2015 Nov;138(Pt 11):3221-37

Citalopram HBr/氢溴酸西肽普兰 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
NCT00363909 Breast Cancer ... 展开 >> Hot Flashes Psychosocial Effects of Cancer and Its Treatment 收起 << Phase 3 Completed - -
NCT03429075 Depressive Disorder, Major Phase 2 Not yet recruiting December 2020 -
NCT00708240 Obsessive Compulsive Disorder Phase 4 Unknown December 2010 Canada, Ontario ... 展开 >> University of Ottawa Institute of Mental Health Research Recruiting Ottawa, Ontario, Canada, K1Z7K4 Contact: Zul Merali, PhD    613-722-6521 ext 6551    zul.merali@rohcg.on.ca    Principal Investigator: Martine F. Flament, MD 收起 <<

Citalopram HBr/氢溴酸西肽普兰 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.

Citalopram HBr/氢溴酸西肽普兰 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.34mL

2.47mL

1.23mL

24.67mL

4.93mL

2.47mL

Citalopram HBr/氢溴酸西肽普兰 技术信息

CAS号59729-32-7
分子式C20H22BrFN2O
分子量 405.3
SMILES Code N#CC1=CC2=C(C(C3=CC=C(F)C=C3)(CCCN(C)C)OC2)C=C1.[H]Br
MDL No. MFCD02101306
别名 氢溴酸西酞普兰 ;Lu 10-171; (±)-Citalopram hydrobromide; Nitalapram; Lu 10-171B; Bonitrile; Citalopram (hydrobromide); Lu 10-171 HBr; Bonitrile HBr; Prepram HBr; Nitalapram HBr; Citalopram hydrobromide
运输蓝冰
InChI Key WIHMBLDNRMIGDW-UHFFFAOYSA-N
Pubchem ID 77995
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, room temperature

溶解方案

DMSO: 40 mg/mL(98.69 mM),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

H2O: 10 mg/mL(24.67 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在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
方案 一
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