Citalopram HBr

Catalog No.S4749 Batch:S474902

Technical Data

Formula	C₂₀H₂₁FN₂O.HBr
Molecular Weight	405.3	CAS No.	59729-32-7
Solubility (25°C)*	In vitro	DMSO	81 mg/mL (199.85 mM)
		Water	15 mg/mL (37.0 mM)
		Ethanol	6 mg/mL (14.8 mM)
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Citalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.

Targets

serotonin reuptake ^[1]
(In rat brain synaptosomal preparations)

1.8 nM

In vitro

Citalopram (Lu 10-171), a new bicyclic phthalane derivative, is an extremely potent inhibitor of neuronal serotonin (5-HT) uptake but has no effect on the uptake of noradrenaline(NA) and dopamine (DA) and no antagonistic activity towards 5-HT, histamine, gamma aminobutyric acid (GABA) and acetylcholine. It is an extremely specific and potent inhibitor of neuronal 5-HT uptake. Uptake mechanisms for other transmitter amines are not influenced by the drug^[1]. The SSRI citalopram has a greater effect on proliferation and a lesser effect on apoptotic activity. It affects cell cycle regulation by increasing proliferative potential and decreasing apoptotic activity in a site specific manner that may be indicative of hyperplasia. Citalopram alters FGF, MSX and TGFB expression in osteoblast cell culture^[3].

In vivo

Citalopram is devoid of cardiotoxic effects even when animals are exposed to concentrations far above the therapeutic level. In man citalopram is metabolized to compounds which are also potent 5-HT-uptake inhibitors without effect on noradrenaline(NA) uptake and which are found in lower concentrations than citalopram itself. Citalopram (1-16 mg/kg) stimulates the hind limb flexor reflex in the spinal rat. Citalopram potentiates 5-HT transmission~ possibly by producing very strong uptake inhibition without simultaneously blocking the post-synaptic 5-HT receptors^[1].

Protocol (from reference)

Cell Assay:^{^[3]}	Cell lines MC3T3-E1 murine calvaria osteoprogenitor cells Concentrations 0.1 nM-100 μM Incubation Time 3 or 7 days Method Cells are cultured in alpha minimum Eagles medium supplemented with 1% penicillin/streptomycin, 10% fetal bovine serum and Amphotericin B. For control data, cells are cultured for 3 or 7 days with standard alpha proliferation media. For SSRI treatments, media is supplemented with citalopram eluted to serially diluted doses between 10⁻⁴ mol through 10⁻¹⁰ mol to achieve a dose response curve.
Animal Study:^{^[2]}	Animal Models Spontaneously Hypertensive rats (SHRs), Lewis (LEW) rats, and Wistar-Kyoto (WKY) rats Dosages 1-10 mg/kg Administration i.p.

Cell Assay:^{^[3]}

Cell lines
MC3T3-E1 murine calvaria osteoprogenitor cells
Concentrations
0.1 nM-100 μM
Incubation Time
3 or 7 days
Method
Cells are cultured in alpha minimum Eagles medium supplemented with 1% penicillin/streptomycin, 10% fetal bovine serum and Amphotericin B. For control data, cells are cultured for 3 or 7 days with standard alpha proliferation media. For SSRI treatments, media is supplemented with citalopram eluted to serially diluted doses between 10⁻⁴ mol through 10⁻¹⁰ mol to achieve a dose response curve.

Animal Study:^{^[2]}

Animal Models
Spontaneously Hypertensive rats (SHRs), Lewis (LEW) rats, and Wistar-Kyoto (WKY) rats
Dosages
1-10 mg/kg
Administration
i.p.

References

Selleck's Citalopram HBr has been cited by 5 publications

Long-term exposure to polypharmacy impairs cognitive functions in young adult female mice [ Aging (Albany NY), 2021, 13(11):14729-14744]	PubMed: 34078751
Inhibitors of Venezuelan Equine Encephalitis Virus Identified Based on Host Interaction Partners of Viral Non-Structural Protein 3 [ Viruses, 2021, 13(8)1533]	PubMed: 34452398
Effect of SSRI exposure on the proliferation rate and glucose uptake in breast and ovary cancer cell lines [ Sci Rep, 2021, 11(1):1250]	PubMed: 33441923
Chronic polypharmacy impairs explorative behavior and reduces synaptic functions in young adult mice [ Aging (Albany NY), 2020, 12(11):10147-10161]	PubMed: 32445552
Chronic Polypharmacy Impairs Explorative Behavior and Reduces Synaptic Functions in Young Adult Mice [ Aging (Albany NY), 2020, 44187]	PubMed: 32445552

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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