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Citalopram HBr 5-HT Receptor inhibitor

Cat.No.S4749

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.
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Quality Control

Batch: Purity: 99.87%
99.87

Solubility

In vitro
Batch:

DMSO : 81 mg/mL (199.85 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 81 mg/mL

Ethanol : 81 mg/mL

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 405.3 Formula

C20H21FN2O.HBr

Storage (From the date of receipt)
CAS No. 59729-32-7 Download SDF Storage of Stock Solutions

Synonyms Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr SMILES CN(C)CCCC1(C2=C(CO1)C=C(C=C2)C#N)C3=CC=C(C=C3)F.Br

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Mechanism of Action

Targets/IC50/Ki
serotonin reuptake
(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. 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.

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.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-12-16)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06433635 ACTIVE_NOT_RECRUITING
Bipolar I Disorder; Depression
Massachusetts General Hospital
2024-10-01 PHASE4
NCT05901571 NOT_YET_RECRUITING
Depressive Disorder, Major
Shanghai 7th People's Hospital
2026-11
NCT06949644 RECRUITING
Delayed Sleep-Wake Phase Disorder
Northwestern University
2025-09-01
NCT05017311 RECRUITING
Major Depressive Disorder
Nova Scotia Health Authority
2023-01-20 PHASE4
NCT05973786 RECRUITING
Bipolar Depression
Dr. Inge Winter
2025-02-11 PHASE3
NCT05603104 RECRUITING
Schizophrenia and Related Disorders; Major Depressive Disorder; Bipolar Depression
Dr. Inge Winter
2025-04-27 PHASE3

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