Vortioxetine (Lu AA21004) HBr
For research use only.
Molecular Weight(MW): 379.36
Vortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM.
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|Description||Vortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM.|
|Features||A multimodal antidepressant.|
Lu-AA21004 inhibits recombinant human CYP1A2, CYP2C9, CYP2D6 and CYP3A4 with IC50 of 40 μM, 39 μM, 9.8 μM and 10 μM, respectively.  Lu AA21004 is a partial h5-HT1B receptor agonist with EC50 of 460 nM and intrinsic activity of 22% using a whole-cell cAMP-based assay. Lu AA21004 binds to the r5-HT7 receptor with a Ki value of 200 nM and is a functional antagonist at the r5-HT7 receptor with an IC50 of 2 μM in an in vitro whole-cell cAMP assay. 
|In vivo||For Lu-AA21004 the hepatic clearances and oral bioavailabilities in rats are found to be 7.1 (L/h)/kg and 16%. Lu-AA21004 (2.5 mg/kg, 5 mg/kg, or 10 mg/kg sc) increases the extracellular levels of 5-HT in the ventral hippocampus in conscious rats. Lu-AA21004 (5 mg/kg, or 10 mg/kg sc) also results in significantly higher basal levels of 5-HT in the medial prefrontal cortex (mPFC) after 3 days of treatment. Lu-AA21004 occupies SERT by 43% and 57% after 3 days of treatment with 5 mg/kg or 10 mg/kg in the rat medial prefrontal cortex.  Lu AA21004 dose-dependent occupies 5-HT1B receptor and the SERT with ED50 of 3.2 mg/kg and 0.4 mg/kg in rats one hour after subcutaneous administration. Lu AA21004 affects the Bezold-Jarisch reflex in the rat dose dependently, inhibiting transient bradycardia with ED50 of 0.11 mg/kg. Lu AA21004 (2.5-10.0 mg/kg s.c.) increases extracellular levels of 5-HT, DA, and NA in the medial prefrontal cortex and in the ventral hippocampus in rats. Lu AA21004 (5 mg/kg s.c.) increases in the extracellular levels of 5-HT (200%) in the ventral hippocampus of rats with 41% occupancy at the SERT. Lu AA21004 (7.8 mg/kg s.c.) significantly decreases the immobility time in the FSL rats but not in the FRL rats. Lu AA21004 (8.0 mg/kg p.o.) produces an increase in social interaction as well as a small, but significant, increase in locomotor activity in rats. Lu AA21004 (7.9 mg/kg s.c.) shows a dose-dependent anxiolytic-like effect in the conditioned fear assay in rats.  Vortioxetine (10 mg/kg) significantly increases freezing 60 min before acquisition in male Sprague-Dawley rats, suggesting enhanced contextual memory formation during acquisition and/or consolidation. Vortioxetine (5 mg/kg) also causes increased freezing rates during retention, an effect that reached statistical significance by post hoc tests. Vortioxetine (2.5 mg/kg or 5 mg/kg) prior to acquisition shows average exploration times of 29s and 33s for the novel object, respectively. Vortioxetine (10 mg/kg) significantly reduces nociception in rats, assessed as increased paw withdrawal latency. Vortioxetine at 5 and 10 mg/kg increases the levels of ACh to 224% and 204% of baseline 20 min after injection. |
|In vitro||DMSO||76 mg/mL (200.33 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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|Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04301492||Recruiting||Drug: Vortioxetine||Depression||IRCCS San Raffaele||January 1 2020||Phase 4|
|NCT03437564||Completed||Drug: Vortioxetine||Healthy Adult Participants||Takeda||February 16 2018||Phase 1|
|NCT02932904||Completed||Drug: Vortioxetine|Drug: Paroxetine|Drug: Placebo||Healthy Volunteers||Takeda||November 21 2016||Phase 4|
|NCT03978286||Completed||Drug: Vortioxetine|Drug: Sertraline||Depression|Type 2 Diabetes Mellitus||Universidad Juárez Autónoma de Tabasco||June 30 2016||Phase 4|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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