| Size | Price | Stock | Qty |
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| 10mg |
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| 100mg |
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| Targets |
Viloxazine targets the norepinephrine transporter (NET) and serotonin (5-HT) receptors. As a NET inhibitor (IC₅₀ = 0.26 μM), it blocks the reuptake of norepinephrine, increasing its concentration in the synaptic cleft. Additionally, Viloxazine is a potent 5-HT2C agonist (EC₅₀ = 32 μM) and 5-HT2B antagonist (IC₅₀ = 27 μM) with a Ki of 4.2 μM for 5-HT2B. The compound also modulates other serotonin receptor subtypes. Its mechanism of action is best explained as a serotonin norepinephrine modulating agent (SNMA), with both serotonergic and noradrenergic components contributing to its psychopharmacological profile.
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| ln Vitro |
In vitro, Viloxazine inhibits norepinephrine reuptake with an IC₅₀ of 0.26 μM. It acts as a potent 5-HT2C agonist (EC₅₀ = 32 μM) and 5-HT2B antagonist (IC₅₀ = 27 μM). The compound's activity at serotonin receptors contributes to its serotonergic modulating properties. In cellular assays, Viloxazine modulates neurotransmitter levels and receptor signaling. Its effects on serotonin and norepinephrine pathways have been characterized in vitro, showing a dual mechanism of action. The hydrochloride salt form improves solubility and stability for experimental applications.
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| ln Vivo |
In vivo, Viloxazine has been studied for its antidepressant and psychopharmacological effects. Its serotonergic and noradrenergic modulating properties contribute to its therapeutic effects in animal models of depression and anxiety. Viloxazine is non-brain-penetrant, suggesting that its effects may be mediated through peripheral mechanisms or through its active metabolites. The compound has been investigated in clinical studies for depression. However, the non-brain-penetrant property is notable and may differentiate it from other antidepressants that require central nervous system penetration.
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| Enzyme Assay |
Non-cell-based assays for Viloxazine include receptor binding studies using membrane preparations from cells expressing human NET, 5-HT2C, or 5-HT2B receptors. Radioligand binding assays are used to measure the affinity (Ki) of Viloxazine for these targets. For NET inhibition, the ability of Viloxazine to inhibit [³H]norepinephrine uptake is measured. For 5-HT receptor activity, functional assays measuring receptor-mediated signaling (e.g., calcium flux, IP3 accumulation, or reporter gene assays) are used to determine agonist or antagonist activity. IC₅₀ and EC₅₀ values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for Viloxazine are performed using cell lines expressing human NET, 5-HT2C, or 5-HT2B receptors. For NET inhibition assays, cells are incubated with [³H]norepinephrine in the presence of Viloxazine, and uptake is measured. For 5-HT2C agonism, cells expressing 5-HT2C receptors are treated with Viloxazine, and intracellular calcium or inositol phosphate accumulation is measured. For 5-HT2B antagonism, cells are stimulated with a 5-HT2B agonist in the presence of Viloxazine, and signaling inhibition is measured. Concentration-response curves are generated to determine IC₅₀ and EC₅₀ values.
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| Animal Protocol |
In vivo experiments with Viloxazine are conducted in animal models of depression, anxiety, or other psychiatric disorders. Rodent models including the forced swim test, tail suspension test, and open field test are used to evaluate antidepressant and anxiolytic effects. Animals are treated with Viloxazine via oral or intraperitoneal administration. Behavior is scored, and neurotransmitter levels in brain or plasma are measured. Pharmacodynamic studies evaluate the compound's effects on serotonin and norepinephrine pathways. The non-brain-penetrant property is evaluated by measuring drug levels in brain tissue.
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| ADME/Pharmacokinetics |
Viloxazine hydrochloride is a non-brain-penetrant compound with characterized pharmacokinetic properties. Following oral administration, the compound is absorbed and distributed primarily in the peripheral circulation. It does not cross the blood-brain barrier to a significant extent. The compound is metabolized in the liver and excreted via urine. Its half-life, bioavailability, and clearance have been characterized in preclinical and clinical studies. The hydrochloride salt form improves aqueous solubility for formulation. PK parameters including Cmax, AUC, and half-life are determined in pharmacokinetic studies.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Currently, no studies have been published regarding the use of vecloxacillin during lactation. If a mother of an older infant requires vecloxacillin, this is not a reason to discontinue breastfeeding, but until more data is available, it is recommended to prioritize other medications, especially when breastfeeding newborns or premature infants. ◉ Effects on Breastfed Infants As of the revision date, no relevant published information was found. ◉ Effects on Lactation and Breast Milk As of the revision date, no relevant published information was found. The toxicity profile of Viloxazine hydrochloride has been evaluated in preclinical and clinical studies. As a serotonin and norepinephrine modulating agent, potential adverse effects include gastrointestinal disturbances, cardiovascular effects (heart rate, blood pressure changes), and central nervous system effects. The compound is non-brain-penetrant, which may reduce the risk of central nervous system side effects compared to centrally acting antidepressants. Comprehensive toxicological studies have been conducted to support clinical development. The compound is generally well-tolerated at therapeutic doses. |
| References | |
| Additional Infomation |
morpholine derivative used as an antidepressant. Its mechanism of action is similar to that of imipramine.
See also: veloxacin (containing the active ingredient). Viloxazine hydrochloride (CAS# 35604-67-2) is a selective norepinephrine transporter (NET) inhibitor (IC₅₀ = 0.26 μM) and serotonin receptor modulator. It is a potent 5-HT2C agonist (EC₅₀ = 32 μM) and 5-HT2B antagonist (IC₅₀ = 27 μM) with a Ki of 4.2 μM for 5-HT2B. The compound's mechanism of action involves serotonergic and noradrenergic pathways, and it is best described as a serotonin norepinephrine modulating agent (SNMA). Viloxazine is used in research on depression and other psychiatric disorders. The compound is also known as Viloxazin hydrochloride and Emovit hydrochloride. As of current knowledge, Viloxazine has been studied in clinical trials but may not be widely approved. |
| Molecular Formula |
C13H20CLNO3
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|---|---|
| Molecular Weight |
273.76
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| Exact Mass |
273.113
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| CAS # |
35604-67-2
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| Related CAS # |
(rac)-Viloxazine-d5 hydrochloride;1276483-10-3;(R)-Viloxazine hydrochloride;56287-63-9;Viloxazine;46817-91-8
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| PubChem CID |
71424
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| Appearance |
White to off-white solid powder
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| Density |
1.061g/cm3
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| Boiling Point |
350.5ºC at 760mmHg
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| Flash Point |
144.3ºC
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| LogP |
2.583
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
18
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| Complexity |
213
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCOC1=CC=CC=C1OCC2CNCCO2.Cl
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| InChi Key |
HJOCKFVCMLCPTP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H19NO3.ClH/c1-2-15-12-5-3-4-6-13(12)17-10-11-9-14-7-8-16-11;/h3-6,11,14H,2,7-10H2,1H3;1H
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| Chemical Name |
2-[(2-ethoxyphenoxy)methyl]morpholine;hydrochloride
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO: 33.33 mg/mL (121.75 mM)
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6528 mL | 18.2642 mL | 36.5283 mL | |
| 5 mM | 0.7306 mL | 3.6528 mL | 7.3057 mL | |
| 10 mM | 0.3653 mL | 1.8264 mL | 3.6528 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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.
Link: https://clinicaltrials.gov/ct2/show/NCT06185985
Conditions:Attention-Deficit/Hyperactivity DisorderLink: https://clinicaltrials.gov/ct2/show/NCT04781140
Conditions:Attention-Deficit/Hyperactivity DisorderLink: https://clinicaltrials.gov/ct2/show/NCT02736656
Conditions:Attention-Deficit/Hyperactivity Disorder
Title:Evaluation of Viloxazine and Its Metabolite 5-Hydroxy-viloxazine Glucuronide Into Breast Milk in Healthy Lactating Women
Status:Completed
updateDate:2024-06-06
Ctid:NCT06259331
Link: https://clinicaltrials.gov/ct2/show/NCT06259331
Conditions:Healthy Lactating WomenLink: https://clinicaltrials.gov/ct2/show/NCT04786990
Conditions:Attention-Deficit/Hyperactivity Disorder (ADHD)Link: https://clinicaltrials.gov/ct2/show/NCT04143217
Conditions:Attention-Deficit/Hyperactivity DisorderLink: https://clinicaltrials.gov/ct2/show/NCT04016779
Conditions:Attention-Deficit/Hyperactivity Disorder (ADHD)Link: https://clinicaltrials.gov/ct2/show/NCT02633527
Conditions:Attention-Deficit/Hyperactivity Disorder (ADHD)Link: https://clinicaltrials.gov/ct2/show/NCT03247543
Conditions:ADHDLink: https://clinicaltrials.gov/ct2/show/NCT03247530
Conditions:ADHDLink: https://clinicaltrials.gov/ct2/show/NCT03247556
Conditions:ADHDLink: https://clinicaltrials.gov/ct2/show/NCT03247517
Conditions:ADHDLink: https://clinicaltrials.gov/ct2/show/NCT04016792
Conditions:ADHDProducts are for research use only; We do not sell to patients
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