| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 1g | |||
| Other Sizes |
| Targets |
Litoxetine targets the serotonin transporter (SERT) and the 5-HT3 receptor. As an SSRI, it inhibits serotonin reuptake, increasing synaptic serotonin levels. As a 5-HT3 receptor antagonist, it binds to brain 5-HT3 receptors with a Ki of 85 nM. The dual mechanism contributes to its antidepressant and antiemetic activities.
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| ln Vitro |
In vitro, litoxetine is a selective serotonin reuptake inhibitor and a 5-HT3 receptor antagonist with a Ki of 85 nM for brain 5-HT3 receptors. Its activity is assessed by measuring serotonin reuptake inhibition in synaptosomal preparations and by measuring 5-HT3 receptor antagonism in receptor binding or functional assays.
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| ln Vivo |
In vivo, litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. At doses of 1 and 10 mg/kg intravenously, litoxetine dose-dependently reduced the number of retching and vomiting episodes and delayed the onset of vomiting. It has been investigated for the treatment of depression and anxiety disorders.
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| Enzyme Assay |
In vitro receptor binding assays for litoxetine measure its affinity for the serotonin transporter and 5-HT3 receptors. Membranes prepared from brain tissue or cells expressing the targets are incubated with radiolabeled ligands and varying concentrations of the compound. A Ki of 85 nM for brain 5-HT3 receptors is determined. Functional assays measure serotonin reuptake inhibition and 5-HT3 receptor antagonism.
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| Cell Assay |
In vitro cell-based assays for litoxetine use cells expressing the serotonin transporter or 5-HT3 receptors. Serotonin reuptake inhibition is measured by assessing the uptake of radiolabeled serotonin. 5-HT3 receptor antagonism is measured by assessing calcium flux or other signaling readouts upon receptor activation.
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| Animal Protocol |
In vivo animal models for litoxetine include ferret models of emesis to assess antiemetic properties. The compound is administered intravenously, and its effects on retching and vomiting are evaluated. Models of depression and anxiety are used to assess antidepressant activity. Pharmacodynamic studies measure serotonin reuptake inhibition and 5-HT3 receptor antagonism.
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| ADME/Pharmacokinetics |
Litoxetine has a molecular formula of C16H19NO and a molecular weight of 241.33 g/mol. It is also known as SL 81.0385 and 4-(naphthalen-2-ylmethoxy)piperidine. The compound is a selective serotonin reuptake inhibitor and 5-HT3 receptor antagonist. It is stored under appropriate conditions for research use.
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| Toxicity/Toxicokinetics |
The toxicity profile of litoxetine is characterized in preclinical safety studies. As an SSRI and 5-HT3 antagonist, common adverse effects may include gastrointestinal disturbances and serotonin-related side effects. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References | |
| Additional Infomation |
Ritoxetine is being investigated in the clinical trial NCT03397771 (DBPC trial, evaluating the safety, tolerability and efficacy of oral Ritoxetine for the treatment of patients with urinary incontinence).
Litoxetine (SL 81.0385) is a selective serotonin reuptake inhibitor (SSRI) and a 5-HT3 receptor antagonist. It binds to brain 5-HT3 receptors with a Ki of 85 nM. Litoxetine acts as an antidepressant and has shown antiemetic properties in ferrets. It is also known as 4-(naphthalen-2-ylmethoxy)piperidine and is used for research purposes in depression and anxiety studies. |
| Molecular Formula |
C16H19NO
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|---|---|
| Molecular Weight |
241.33
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| Exact Mass |
241.147
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| CAS # |
86811-09-8
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| PubChem CID |
65650
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1g/cm3
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| Boiling Point |
387.1ºC at 760 mmHg
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| Flash Point |
159.2ºC
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| Index of Refraction |
1.607
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| LogP |
3.437
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
250
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O(CC1C=CC2C=CC=CC=2C=1)C1CCNCC1
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| InChi Key |
MJJDYOLPMGIWND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H19NO/c1-2-4-15-11-13(5-6-14(15)3-1)12-18-16-7-9-17-10-8-16/h1-6,11,16-17H,7-10,12H2
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| Chemical Name |
4-(naphthalen-2-ylmethoxy)piperidine
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| Synonyms |
Litoxetinum; Litoxetina; Litoxetine
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1437 mL | 20.7185 mL | 41.4370 mL | |
| 5 mM | 0.8287 mL | 4.1437 mL | 8.2874 mL | |
| 10 mM | 0.4144 mL | 2.0719 mL | 4.1437 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.
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