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。


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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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| 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 |
| 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 << |
| 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 |
|
| 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 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
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