| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Vortioxetine acts as an antagonist at 5‑HT3A and 5‑HT7 receptors and as an agonist/partial agonist at 5‑HT1A and 5‑HT1B receptors. It also inhibits the serotonin transporter (SERT). The reported Ki values are 15 nM for 5‑HT1A, 33 nM for 5‑HT1B, 3.7 nM for 5‑HT3A, 19 nM for 5‑HT7, and 1.6 nM for SERT.
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| ln Vitro |
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Vortioxetine‑d8 hydrobromide itself is primarily used as a tracer; therefore, in vitro activity is not directly measured. The parent compound vortioxetine modulates extracellular serotonin levels through combined SERT inhibition and receptor modulation. Cellular assays using serotonergic neurons demonstrate that vortioxetine increases serotonin release and alters firing patterns of raphe nucleus neurons. |
| ln Vivo |
In animal models, vortioxetine exhibits antidepressant‑like effects in forced swim tests and tail suspension tests. Chronic administration alters serotonin receptor density and restores stress‑induced neurogenesis deficits. The deuterated form is assumed to retain these in vivo activities and is used as a stable isotope standard in quantitative pharmacokinetic studies.
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| Enzyme Assay |
A typical binding assay uses radiolabeled ligands and membrane preparations from HEK‑293 cells expressing human recombinant serotonin receptors or SERT. Vortioxetine‑d8 is incubated with the receptor source, and bound radioactivity is measured after filtration. Non‑specific binding is defined using excess non‑labeled vortioxetine. Ki values are calculated by non‑linear regression.
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| Cell Assay |
For cellular assays, serotonergic neurons or heterologous cells expressing SERT are treated with vortioxetine‑d8 (0.1 nM‑10 uM). After incubation, serotonin uptake is measured by adding tritiated serotonin and counting accumulated radioactivity. Alternatively, receptor‑mediated calcium flux or cAMP changes are measured with fluorescent indicators.
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| Animal Protocol |
The deuterated compound is generally administered intraperitoneally or orally to rodents. Plasma and brain tissue samples are collected at various time points, processed, and analyzed by LC‑MS/MS. The substitution with eight deuterium atoms provides a distinct mass shift, allowing precise quantification of the non‑deuterated vortioxetine when the labeled variant is used as an internal standard.
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| ADME/Pharmacokinetics |
Vortioxetine‑d8 hydrobromide has the same physicochemical properties as the non‑deuterated drug, with increased metabolic stability due to the deuterium isotope effect, which can slow CYP‑mediated metabolism. However, when used as an internal standard at trace levels, its own pharmacokinetic profile is negligible.
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| Toxicity/Toxicokinetics |
Vortioxetine hydrobromide is generally well‑tolerated in humans. Common side effects include nausea, headache, and dizziness. The deuterated version is not intended for human use. However, its use as an internal standard does not raise additional safety concerns.
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| References | |
| Additional Infomation |
Vortioxetine (Lu AA21004) received FDA approval in September 2013 for the treatment of major depressive disorder (MDD). Its unique multimodal mechanism distinguishes it from selective serotonin reuptake inhibitors (SSRIs). Vortioxetine also shows procognitive effects in MDD patients and is being studied for generalized anxiety disorder. The deuterated form is a valuable analytical tool for pharmacokinetic studies and therapeutic drug monitoring.
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| Molecular Formula |
C18H15D8BRN2S
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|---|---|
| Related CAS # |
Vortioxetine hydrobromide;960203-27-4
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| Appearance |
Typically exists as solid at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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