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| Targets |
The primary target of Norfluoxetine is the serotonin transporter (SERT), a membrane protein responsible for the reuptake of serotonin from the synaptic cleft back into the presynaptic neuron. By inhibiting SERT, norfluoxetine increases the concentration of serotonin in the synaptic cleft, enhancing serotonergic neurotransmission. This mechanism is responsible for the antidepressant effects of fluoxetine and its active metabolite. Norfluoxetine is a potent and selective SERT inhibitor, with significantly lower affinity for norepinephrine and dopamine transporters.
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| ln Vitro |
In vitro, Norfluoxetine is a potent and selective inhibitor of the serotonin transporter (SERT). Its activity is typically measured using radioligand binding assays with cell membranes expressing SERT, and functional assays that measure serotonin uptake inhibition in synaptosomes or cell lines expressing SERT. IC50 values are determined from dose-response curves. The compound's selectivity for SERT over norepinephrine and dopamine transporters is assessed to confirm its specificity. Norfluoxetine also has weak activity at various other receptors, including 5-HT2C, which may contribute to its side-effect profile.
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| ln Vivo |
Pentylenetetrazole has been shown to have a considerable protective effect against epilepsy-induced seizures. Pretreatment with fluoxetine or norfluoxetine hydrochloride (20 mg/kg sc), as well as phenytoin (30 mg/kg sc) and clonazepam (0.1 mg/kg sc), considerably enhanced survival rate and duration [1].
In vivo, Norfluoxetine is the primary active metabolite of fluoxetine and contributes to its antidepressant effects. It has a longer half-life than fluoxetine (approximately 7-15 days for norfluoxetine vs. 1-3 days for fluoxetine), which allows for once-daily dosing and provides a buffer against missed doses. The compound's prolonged action is due to its high protein binding and slow elimination. Norfluoxetine's effects on serotonin levels in the brain have been demonstrated in microdialysis studies. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Norfluoxetine involve radioligand binding studies using cell membranes expressing the serotonin transporter (SERT). Competitive binding assays are performed using a radiolabeled SERT ligand (e.g., [3H]paroxetine or [3H]citalopram) to determine the compound's affinity (Ki) for the transporter. Selectivity profiling against norepinephrine and dopamine transporters, as well as various serotonin receptor subtypes (5-HT1A, 5-HT2A, 5-HT2C, etc.), is performed to assess the compound's specificity. Functional assays that measure serotonin uptake inhibition are employed to confirm the compound's inhibitory activity.
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| Cell Assay |
In vitro cellular assays for Norfluoxetine are conducted in cell lines expressing SERT, such as HEK293 cells transfected with SERT, or in synaptosomal preparations. Cells or synaptosomes are treated with varying concentrations of norfluoxetine, and serotonin uptake is measured using radiolabeled serotonin ([3H]5-HT). The compound's ability to inhibit serotonin uptake is quantified. These assays confirm that norfluoxetine engages its target in a cellular context and produces the expected inhibition of serotonin reuptake.
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| Animal Protocol |
In vivo animal studies for Norfluoxetine are conducted in animal models of depression, such as the forced swim test or tail suspension test. Animals are administered the compound orally or intraperitoneally, and antidepressant-like effects are assessed. Microdialysis studies are performed to measure extracellular serotonin levels in the brain. Pharmacokinetic studies are performed to determine the compound's half-life, bioavailability, and tissue distribution. These studies confirm that norfluoxetine is effective in vivo and provide information about its pharmacokinetic properties.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Norfluoxetine indicate that it has a molecular weight of 345.77 and a molecular formula of C17H16F3NO·HCl. The compound is the active metabolite of fluoxetine with a longer half-life (approximately 7-15 days). It is highly protein-bound (approximately 94.5%) and is extensively distributed in tissues. The compound is metabolized in the liver primarily by CYP2D6 and other cytochrome P450 enzymes. For storage, the powder should be kept under appropriate conditions to maintain stability.
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| Toxicity/Toxicokinetics |
Toxicological information for Norfluoxetine is derived from its clinical use as the active metabolite of fluoxetine. Common side effects include nausea, headache, insomnia, and sexual dysfunction. Serious adverse events include serotonin syndrome, gastrointestinal bleeding, and hyponatremia. The compound is contraindicated with MAO inhibitors and should be used with caution in patients with liver disease or a history of seizures.
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| References |
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| Additional Infomation |
Norfluoxetine Hydrochloride is the primary active metabolite of the SSRI antidepressant fluoxetine. It is a potent and selective inhibitor of the serotonin transporter (SERT) and contributes to the therapeutic effects of fluoxetine. Norfluoxetine has a longer half-life than fluoxetine. It is available from research chemical suppliers for research purposes.
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| Molecular Formula |
C16H16NOF3.HCL
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| Molecular Weight |
331.76048
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| Exact Mass |
331.095
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| CAS # |
57226-68-3
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| Related CAS # |
Norfluoxetine-d5 hydrochloride;1188265-34-0
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| PubChem CID |
151371
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| Appearance |
White to off-white solid powder
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| Density |
1.204g/cm3
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| Boiling Point |
381.1ºC at 760 mmHg
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| Flash Point |
184.3ºC
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| LogP |
5.676
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
294
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GMTWWEPBGGXBTO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H16F3NO.ClH/c17-16(18,19)13-6-8-14(9-7-13)21-15(10-11-20)12-4-2-1-3-5-12;/h1-9,15H,10-11,20H2;1H
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| Chemical Name |
3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine;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 : ~125 mg/mL (~376.78 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 | 3.0142 mL | 15.0711 mL | 30.1423 mL | |
| 5 mM | 0.6028 mL | 3.0142 mL | 6.0285 mL | |
| 10 mM | 0.3014 mL | 1.5071 mL | 3.0142 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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