2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Viloxazine hydrochloride

Viloxazine hydrochloride  (Synonyms: Viloxazin hydrochloride; Emovit hydrochloride)

Cat. No.: HY-125784 Purity: 98.94%
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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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Viloxazine hydrochloride Chemical Structure

Viloxazine hydrochloride Chemical Structure

CAS No. : 35604-67-2

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Based on 1 publication(s) in Google Scholar

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Description

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)[1][2][3].

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%). In cell experiments, the IC50 values were 0.26 μM (NET), 257 μM (SERT), 27 μM (5-HT2B), 68 μM (ADRβ2), and 93 μM (ADRα1B), respectively, and it showed significant kinase agonist activity with an EC50 of 32 μM (5-HT2C)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Viloxazine hydrochloride Related Antibodies
In Vivo

Viloxazine hydrochloride (50 mg/kg; i.p.; single injection) significantly increases NE, DA, and 5-HT levels in the prefrontal cortex (PFC), nucleus accumbens (Acb), and amygdala (Amg) in Sprague-Dawley rats[1].
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.

Animal Model: Sprague-Dawley rats (male, 300-400 g, 7-8 weeks; naïve model)[1]
Dosage: 50 mg/kg (0.9% NaCl)
Administration: Intraperitoneal injection, single
Result: Increased extracellular NE, DA, and 5-HT in the PFC, Acb, and Amg. Resulted peak responses at 60 min post-injection (NE: 649% ± 57%, DA: 670% ± 105%, 5-HT: 506% ± 133% of baseline).
Animal Model: Sprague-Dawley rats (male, 300-400 g, 7-8 weeks; naïve model)[2]
Dosage: 1, 3, 10, 30 mg/kg (0.9% NaCl)
Administration: Intraperitoneal injection, single dose.
Result: Dose-dependently increased NE (30 mg/kg: 545% ± 78% of baseline) and 5-HT (30 mg/kg: 197.9% ± 46.0% of baseline) in the PFC.
Decreased DHPG levels significantly at 10 and 30 mg/kg (p<0.05), without changed DA levels.
Molecular Weight

273.76

Formula

C13H20ClNO3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCOC1=C(OCC2OCCNC2)C=CC=C1.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

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Purity & Documentation

Purity: 98.94%

SDS (393 KB)

COA (250 KB) HNMR (243 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References

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 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
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Viloxazine hydrochloride Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Viloxazine35604-67-2ViloxazinEmovit5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorSerotonergicnoradrenergic5-HTdepressionInhibitorinhibitorinhibit

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