Vortioxetine (Lu AA21004) HBr
For research use only.
CAS No. 960203-27-4
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
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|% DMSO % % Tween 80 % ddH2O|
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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.
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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|
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