Viloxazine hydrochloride
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Viloxazine hydrochloride 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).
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- Pureté : 99.46%
- CAS No.: 35604-67-2
- Formule: C13H20ClNO3
- Masse moléculaire:273.76
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
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5-HT2B Receptor |
5-HT2C Receptor |
In Vitro
Viloxazine hydrochloride (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.
In Vivo
Viloxazine hydrochloride (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 hydrochloride 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, without changed DA levels.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 35604-67-2
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Appearance Solid
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Masse moléculaire 273.76
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Formule C13H20ClNO3
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Color White to off-white
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SMILES
CCOC1=C(OCC2OCCNC2)C=CC=C1.Cl
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Synonyms
Viloxazin hydrochloride; Emovit hydrochloride
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
In Vitro:
H2O : 40 mg/mL (146.11 mM; Need ultrasonic)
DMSO : 33.33 mg/mL (121.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (278 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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 (sealed storage, away from moisture). 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 / H2O | 1 mM | 3.6528 mL | 18.2642 mL | 36.5283 mL | 91.3209 mL |
| 5 mM | 0.7306 mL | 3.6528 mL | 7.3057 mL | 18.2642 mL | |
| 10 mM | 0.3653 mL | 1.8264 mL | 3.6528 mL | 9.1321 mL | |
| 15 mM | 0.2435 mL | 1.2176 mL | 2.4352 mL | 6.0881 mL | |
| 20 mM | 0.1826 mL | 0.9132 mL | 1.8264 mL | 4.5660 mL | |
| 25 mM | 0.1461 mL | 0.7306 mL | 1.4611 mL | 3.6528 mL | |
| 30 mM | 0.1218 mL | 0.6088 mL | 1.2176 mL | 3.0440 mL | |
| 40 mM | 0.0913 mL | 0.4566 mL | 0.9132 mL | 2.2830 mL | |
| 50 mM | 0.0731 mL | 0.3653 mL | 0.7306 mL | 1.8264 mL | |
| 60 mM | 0.0609 mL | 0.3044 mL | 0.6088 mL | 1.5220 mL | |
| 80 mM | 0.0457 mL | 0.2283 mL | 0.4566 mL | 1.1415 mL | |
| 100 mM | 0.0365 mL | 0.1826 mL | 0.3653 mL | 0.9132 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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