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Vortioxetine

In stock
Catalog No.
A3926
5-HT receptors antagonist
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$110.00
In stock
5mg
$100.00
In stock
25mg
$350.00
In stock
100mg
$1,200.00
In stock

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Background

Vortioxetine is a novel multimodal antidepressant currently under development for the treatment of MDD. The serotonergic system plays an important role in cognitive functions via various 5-HT receptors.

In vitro: Vortioxetine (Lu AA21004) was the lead compound, displaying high affinity for recombinant human 5-HT1A (Ki = 15 nM), 5-HT1B (Ki = 33 nM), 5-HT3A (Ki = 3.7 nM), 5-HT7 (Ki = 19 nM), and noradrenergic β1 (Ki = 46 nM) receptors, and SERT (Ki = 1.6 nM). Vortioxetine displayed antagonistic properties at 5-HT3A and 5-HT7 receptors, partial agonist properties at 5-HT1B receptors, agonistic properties at 5-HT1A receptors, and potent inhibition of SERT [1].

In vivo: In conscious rats, vortioxetine significantly increased extracellular 5-HT levels in the brain after acute and 3 days of treatment. Following the 3-day treatment (5 or 10 mg/kg/day) SERT occupancies were only 43% and 57%, respectively [1].

Clinical trial: Drugs were administered in the evening of 15 consecutive days. Vortioxetine did not cause cognitive or psychomotor impairment. However, mirtazapine impaired cognitive and psychomotor performance on day 2. Most of these effects disappeared after multiple doses of mirtazapine [2].

References:
[1] Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB.  Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder. J Med Chem. 2011;54(9):3206-21.
[2] Theunissen EL, Street D, Højer AM, Vermeeren A, van Oers A, Ramaekers JG.  A randomized trial on the acute and steady-state effects of a new antidepressant, vortioxetine (Lu AA21004), on actual driving and cognition. Clin Pharmacol Ther. 2013;93(6):493-501.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt298.45
Cas No.508233-74-7
FormulaC18H22N2S
SynonymsLu AA 21004;Lu AA21004
Solubility≥14.9 mg/mL in DMSO, ≥4.31 mg/mL in EtOH with ultrasonic, <2.51 mg/mL in H2O
Chemical Name1-[2-(2,4-dimethylphenyl)sulfanylphenyl]piperazine
SDFDownload SDF
Canonical SMILESCC1=CC(=C(C=C1)SC2=CC=CC=C2N3CCNCC3)C
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description Vortioxetine is an antagonist of 5-HT3 receptor with IC50 value of 12 nM.
Targets 5-HT3 receptor          
IC50 12 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

Vortioxetine