Viloxazine
Viloxazine is a non-brain-penetrant, selective norepinephrine transporter (NET) inhibitor (IC50= 0.26 μM) and 5-HT receptor modulator. Viloxazine antagonizes 5-HT2B receptors (Ki=4.2 μM) and agonizes 5-HT2C receptors (EC50= 32 μM), respectively, and enhances 5-HT neurotransmission by modulating 5-HT2B/C receptors. Viloxazine also competitively inhibits NET from increasing NE and DA levels in the synaptic cleft, and can be used in the study of attention deficit hyperactivity disorder (ADHD).
For research use only. We do not sell to patients.
- Purity: 99.15%
- CAS No.: 46817-91-8
- Formula: C13H19NO3
- Molecular Weight:237.29
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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All 5-HT Receptor Isoforms
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Biological Activity
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5-HT2B Receptor |
5-HT2C Receptor |
Viloxazine (10 μM; kinase binding assay) significantly inhibits 7 out of 132 targets, including NET, 5-HT2B, 5-HT2C, 5-HT1B, 5-HT7, ADRα1A, ADRα1B receptors, with the highest selectivity for NET (inhibition rate>50%)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Viloxazine (1-30 mg/kg; i.p.; single injection) dose-dependently increases NE and 5-HT levels in the PFC and inhibited the NE metabolite DHPG in Sprague-Dawley rats, but had no significant effect on DA[2].
The median lethal dose (LD50) of Viloxazine in different animals is 500-1000 mg/kg (po, mouse), 2000 mg/kg (po, rat), and 60 mg/kg (iv, mouse)[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rats (male, 300-400 g, 7-8 weeks; naïve model)[1]
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Dosage:50 mg/kg (0.9% NaCl)
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Administration:Intraperitoneal injection, single
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Result:Increased extracellular NE, DA, and 5-HT in the PFC, Acb, and Amg. Resulted peak responses at 60 min post-injection (NE: 649%, DA: 670%, 5-HT: 506% of baseline).
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Animal Model:Sprague-Dawley rats (male, 300-400 g, 7-8 weeks; naïve model)[2]
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Dosage:1, 3, 10, 30 mg/kg (0.9% NaCl)
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Administration:Intraperitoneal injection, single dose
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Result:Dose-dependently increased NE (30 mg/kg: 545% of baseline) and 5-HT (30 mg/kg: 197.9% of baseline) in the PFC.
Decreased DHPG levels significantly at 10 and 30 mg/kg (p<0.05), without changed DA levels.
Chemical Information
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CAS No. 46817-91-8
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Appearance Liquid (Density: 1.062±0.06 g/cm3)
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Molecular Weight 237.29
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Formula C13H19NO3
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Color Colorless to light yellow
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SMILES
CCOC1=C(C=CC=C1)OCC2OCCNC2
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Synonyms
Viloxazin; Emovit
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : ≥ 120 mg/mL (505.71 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (12.64 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (12.64 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Yu C, et al. New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300. [Content Brief]
[2]. Garcia-Olivares J, et al. Viloxazine Increases Extracellular Concentrations of Norepinephrine, Dopamine, and Serotonin in the Rat Prefrontal Cortex at Doses Relevant for the Treatment of Attention-Deficit/Hyperactivity Disorder. J Exp Pharmacol. 2024 Jan 16;16:13-24. [Content Brief]
[3]. Findling RL, et al. Viloxazine in the Management of CNS Disorders: A Historical Overview and Current Status. CNS Drugs. 2021 Jun;35(6):643-653. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.2143 mL | 21.0713 mL | 42.1425 mL | 105.3563 mL |
| 5 mM | 0.8429 mL | 4.2143 mL | 8.4285 mL | 21.0713 mL | |
| 10 mM | 0.4214 mL | 2.1071 mL | 4.2143 mL | 10.5356 mL | |
| 15 mM | 0.2810 mL | 1.4048 mL | 2.8095 mL | 7.0238 mL | |
| 20 mM | 0.2107 mL | 1.0536 mL | 2.1071 mL | 5.2678 mL | |
| 25 mM | 0.1686 mL | 0.8429 mL | 1.6857 mL | 4.2143 mL | |
| 30 mM | 0.1405 mL | 0.7024 mL | 1.4048 mL | 3.5119 mL | |
| 40 mM | 0.1054 mL | 0.5268 mL | 1.0536 mL | 2.6339 mL | |
| 50 mM | 0.0843 mL | 0.4214 mL | 0.8429 mL | 2.1071 mL | |
| 60 mM | 0.0702 mL | 0.3512 mL | 0.7024 mL | 1.7559 mL | |
| 80 mM | 0.0527 mL | 0.2634 mL | 0.5268 mL | 1.3170 mL | |
| 100 mM | 0.0421 mL | 0.2107 mL | 0.4214 mL | 1.0536 mL |
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