Citalopram
Based on 9 publication(s) in Google Scholar
Citalopram is a racemate mixture of the active S(+)-enantiomer (Escitalopram; HY-14258) and R(-)-enantiomer. Citalopram is an orally active selective serotonin reuptake inhibitor (SSRI). Citalopram is an antidepressant and enhances serotoninergic neurotransmission.
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 59729-33-8
- Formula: C20H21FN2O
- Molecular Weight:324.39
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Citalopram
More- J Med Chem. 2026 Feb 10. [Abstract]
- Eur J Pharmacol. 2018 Dec 15:841:57-66. [Abstract]
- Comput Struct Biotechnol J. 2023 Jul 7:21:3490-3502. [Abstract]
- Neurochem Int. 2019 Dec;131:104552. [Abstract]
- ACS Chem Neurosci. 2025 Jun 18;16(12):2312-2321. [Abstract]
- J Clin Psychopharmacol. 2021 Sep-Oct;41(5):525-533. [Abstract]
- Pharmacol Res Perspect. 2020 Apr;8(2):e00575. [Abstract]
- Orebro University. 2024.
- Research Square Preprint. 2021 Feb.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>200 μM
Compound: Citalopram
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Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human HEK293 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 32388114] |
| HEK293 | IC50 |
0.019 μM
Compound: Citalopram
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Inhibition of [3H]-serotonin reuptake at human SERT expressed in HEK293 cells after 15 to 20 mins by fluorescence neurotransmitter transporter assay
Inhibition of [3H]-serotonin reuptake at human SERT expressed in HEK293 cells after 15 to 20 mins by fluorescence neurotransmitter transporter assay
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[PMID: 21227702] |
| HEK293 | IC50 |
18.8 μM
Compound: citalopram
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Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy
|
[PMID: 18788725] |
| HEK293 | IC50 |
3.17 nM
Compound: citalopram
|
Inhibition of [3H]5-HT reuptake at rat SERT expressed in HEK293 cells after 2 mins by liquid scintillation counting
Inhibition of [3H]5-HT reuptake at rat SERT expressed in HEK293 cells after 2 mins by liquid scintillation counting
|
[PMID: 19717215] |
| SH-SY5Y | IC50 |
>200 μM
Compound: Citalopram
|
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
|
[PMID: 32388114] |
| Ventricular myocyte | IC50 |
64.5 μM
Compound: Citalopram
|
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes
|
[PMID: 22761000] |
Citalopram (25-175 μM; 24 h) shows a concentration-dependent cytotoxicity[3].
Citalopram (100 μM; 24 h) strongly down-regulates MYBL2, BIRC5, BARD1, AURKA, CCNA2 and CCNE1 in B104 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Rat B104, human SH-SY5Y, IMR32 and Kelly neuroblastoma cells
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Concentration:25, 50, 100, 125, 150, 175 μM
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Incubation Time:24 h
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Result:Showed a concentration-dependent cytotoxicity.
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Cell Line:B104 cells
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Concentration:100 μM
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Incubation Time:24 h
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Result:Strongly down-regulated MYBL2, BIRC5, BARD1, AURKA, CCNA2 and CCNE1 in B104 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J and DBA/2J mice, aged 5-7 weeks, 16-20 g[4]
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Dosage:5-40 mg/kg
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Administration:IP
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Result:Reduced immobility time in DBA/2J mice but not in C57BL/6J mice.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 59729-33-8
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Appearance Solid
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Molecular Weight 324.39
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Formula C20H21FN2O
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Color White to off-white
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SMILES
N#CC1=CC=C2C(CCCN(C)C)(OCC2=C1)C3=CC=C(C=C3)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (9)
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Journal Impact Factor
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Most Recent
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J Med Chem
Bioisostere-Driven Discovery of SePP: A Selenium-Containing Polypharmacological Agent Relevant to Fragile X Syndrome. [Abstract]2026 Feb 10. PMID: 41666325 -
Eur J Pharmacol
Effects of noradrenergic and serotonergic systems on risk-based decision-making and center arena activity in open field in rats. [Abstract]2018 Dec 15:841:57-66. PMID: 30268663 -
Comput Struct Biotechnol J
Drug repurposing screens to identify potential drugs for chronic kidney disease by targeting prostaglandin E2 receptor. [Abstract]2023 Jul 7:21:3490-3502. PMID: 37484490 -
Neurochem Int
Selectivity of (±)-citalopram at nicotinic acetylcholine receptors and different inhibitory mechanisms between habenular α3β4* and α9α10 subtypes. [Abstract]2019 Dec;131:104552. PMID: 31545995 -
ACS Chem Neurosci
Tyrosine: A Key Neurotransmitter in Selective Serotonin Reuptake Inhibitor Treatment for Chronic Restraint Stress-Induced Reduction of Intestinal Innate Lymphoid Cell Type 3 Cells. [Abstract]2025 Jun 18;16(12):2312-2321. PMID: 40468180 -
J Clin Psychopharmacol
Citalopram and Cannabidiol: In Vitro and In Vivo Evidence of Pharmacokinetic Interactions Relevant to the Treatment of Anxiety Disorders in Young People. [Abstract]2021 Sep-Oct;41(5):525-533. PMID: 34121064 -
Pharmacol Res Perspect
Applicability of free drug hypothesis to drugs with good membrane permeability that are not efflux transporter substrates: A microdialysis study in rats. [Abstract]2020 Apr;8(2):e00575. PMID: 32266794 -
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Solvent & Solubility
DMSO : 100 mg/mL (308.27 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (7.71 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (279 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
[1]. Carlsson B, et al. Enantioselective analysis of citalopram and escitalopram in postmortem blood together with genotyping for CYP2D6 and CYP2C19. J Anal Toxicol. 2009;33(2):65-76. [Content Brief]
[2]. Milne RJ, et al. Citalopram. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in depressive illness. Drugs. 1991;41(3):450-477. [Content Brief]
[3]. 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. [Content Brief]
[4]. Zeng-Liang Jin, et al. Mouse strain differences in SSRI sensitivity correlate with serotonin transporter binding and function. Sci Rep. 2017 Aug 17;7(1):8631. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0827 mL | 15.4135 mL | 30.8271 mL | 77.0677 mL |
| 5 mM | 0.6165 mL | 3.0827 mL | 6.1654 mL | 15.4135 mL | |
| 10 mM | 0.3083 mL | 1.5414 mL | 3.0827 mL | 7.7068 mL | |
| 15 mM | 0.2055 mL | 1.0276 mL | 2.0551 mL | 5.1378 mL | |
| 20 mM | 0.1541 mL | 0.7707 mL | 1.5414 mL | 3.8534 mL | |
| 25 mM | 0.1233 mL | 0.6165 mL | 1.2331 mL | 3.0827 mL | |
| 30 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5689 mL | |
| 40 mM | 0.0771 mL | 0.3853 mL | 0.7707 mL | 1.9267 mL | |
| 50 mM | 0.0617 mL | 0.3083 mL | 0.6165 mL | 1.5414 mL | |
| 60 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL | |
| 80 mM | 0.0385 mL | 0.1927 mL | 0.3853 mL | 0.9633 mL | |
| 100 mM | 0.0308 mL | 0.1541 mL | 0.3083 mL | 0.7707 mL |