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Tianeptine Sulfate Capsules are oral capsule formulations containing the active ingredient Tianeptine Sulfate, and are a type of antidepressant. Teneprone sulfate is the sulfate form of Teneprone, which has higher chemical stability and a half-life (approximately 6 hours) longer than the sodium salt form (Tianeptine Sodium, with a half-life of approximately 2.5 hours). Enhancing 5-hydroxytryptamine (5-HT) reuptake: Unlike traditional antidepressants such as SSRIs that inhibit reuptake, tianeptone improves mood by promoting 5-HT reuptake. Regulating the glutamatergic system may alleviate depressive symptoms and promote neuroplasticity through NMDA receptor antagonism. Partial activation of μ - opioid receptors can produce mild analgesic and anti anxiety effects, but the risk of dependence is lower than that of traditional opioid drugs. Tenafenone itself has a bitter taste, and the capsule can avoid direct contact with the oral cavity, improving patient compliance. Each capsule contains a fixed dose (such as 12.5mg or 25mg) for easy control of dosage. The capsule shell can prevent the degradation of drugs in stomach acid, ensuring the release of active ingredients in the intestine.
Our products
| Product Name | Tianeptine Sulfate Powder | Tianeptine Sulfate Tablets | Tianeptine Sulfate Capsules |
| Product Type | Powder | Tablet | Capsules |
| Product Purity | ≥99% | ≥99% | ≥99% |
| Product Specifications | 100g/1kg/etc. | 10mg/25mg/30mg | 10mg/25mg/30mg |
| Product Form | Organic synthesis | Take Orally | Take Orally |
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Tianeptine Sulfate COA
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| Certificate of Analysis | ||
| Compound name | Tianeptine Sulfate | |
| Grade | Pharmaceutical grade | |
| CAS No. | 1224690-84-9 | |
| Quantity | 337.3kg | |
| Packaging standard | 25kg/drum | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
| Lot No. | 202501090032 | |
| MFG | Jan 9th 2025 | |
| EXP | Jan 8th 2028 | |
| Structure |
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| Item | Enterprise standard | Analysis result |
| Appearance | White or almost white powder | Conformed |
| Water content | ≤5.0% | 0.38% |
| Loss on drying | ≤1.0% | 0.27% |
| Heavy Metals | Pb≤0.5ppm | N.D. |
| As≤0.5ppm | N.D. | |
| Hg≤0.5ppm | N.D. | |
| Cd≤0.5ppm | N.D. | |
| Purity (HPLC) | ≥99.0% | 99.80% |
| Single impurity | <0.8% | 0.43% |
| Total microbial count | ≤750cfu/g | 70 |
| E. Coli | ≤2MPN/g | N.D. |
| Salmonella | N.D. | N.D. |
| Ethanol (by GC) | ≤5000ppm | 400ppm |
| Storage | Store in a sealed, dark, and dry place below 2-8°C | |
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Cross species mechanism of action
Tianeptin Sulfate Capsules is the sulfate form of Tianeptin ketone. As an antidepressant, its mechanism of action differs from traditional selective serotonin reuptake inhibitors (SSRIs) or tricyclic antidepressants (TCAs). Traditional antidepressants often exert their effects by inhibiting the reuptake of 5-HT or norepinephrine (NE), while Tianeptin Sulfate enhances 5-HT reuptake, regulates the glutamatergic system, and partially activates μ - opioid receptors to produce antidepressant, anti anxiety, and neuroprotective effects. Cross species research is an important method in drug development and neuroscience. By comparing the responses of different species (such as humans, rodents, and non-human primates) to drugs, the conservation and species specificity of the mechanism of action can be revealed, providing a bridge for the translation of preclinical research into clinical practice.
Pharmacological properties
Chemical Structure and Pharmacokinetics
Tianeptin Sulfate is a sulfate complex of Tianeptin, which has better chemical stability than its sodium salt form (Tianeptin Sodium), with a half-life of about 6 hours (sodium salt about 2.5 hours), and is suitable for 1-2 doses per day. Its oral bioavailability is about 99%, metabolized as inactive metabolites in the liver, and excreted through the kidneys.
The 5-hydroxytryptamine (5-HT) system: It enhances 5-HT reuptake in brain regions such as the hippocampus and prefrontal cortex, reduces synaptic gap 5-HT concentration, but long-term use can upregulate 5-HT1A receptor sensitivity and improve emotional regulation.
Glutamic acid system: regulates NMDA receptor function, inhibits excessive release of glutamate, reduces excitotoxicity, and promotes neuroplasticity (such as neurogenesis in hippocampus).
μ - opioid receptors: Partial activation of μ - opioid receptors produces mild analgesic and anti anxiety effects, but the risk of dependence is lower than traditional opioid drugs (such as morphine).
Clinical and neuroimaging evidence
Multiple randomized controlled trials (RCTs) have shown that Tianeptine Sulfate (12.5-25 mg/day) can significantly improve Hamilton Depression Rating Scale (HAMD) scores in patients with depression, with efficacy comparable to SSRIs (such as fluoxetine), but with faster onset (1-2 weeks vs. 2-4 weeks) and fewer side effects such as sexual dysfunction and weight gain.
5-HT system: Functional magnetic resonance imaging (fMRI) shows that can enhance the functional connectivity between the prefrontal cortex and the limbic system, and improve the emotional regulation network.
Glutamate energy system: Magnetic resonance spectroscopy (MRS) studies have found that the concentration of glutamate in the hippocampus decreases after treatment, indicating that excessive release of glutamate is inhibited.
Neuroplasticity: Long term treatment can increase hippocampal volume (measured by MRI), which is associated with improved cognitive function. Although direct evidence of μ - opioid receptor activation in human studies is limited, some patients
Research on Rodents (Mice, Rats): Mechanism Validation and Dose Effect Analysis
Forced swimming test (FST): Tianeptin Sulfate Capsules (5-20 mg/kg, oral) can significantly shorten immobility time in mice/rats, indicating antidepressant effects.
Elevated Cross Maze (EPM): Increasing open arm exploration time indicates anti anxiety effects.
Chronic Unpredictable Stress (CUS) Model: Reversing Stress Induced Decreased Sugar Preference, Weight Loss, and Cognitive Impairment.
5-HT system: Microdialysis studies have shown that Tianeptin Sulfate (10 mg/kg) can rapidly increase hippocampal 5-HT reuptake and reduce synaptic gap 5-HT concentration, consistent with human studies. Long term use upregulates 5-HT1A receptor expression and enhances receptor sensitivity.
Glutamate system: inhibits hippocampal glutamate release, reduces NMDA receptor activation, and alleviates excitotoxicity. Promote the expression of brain-derived neurotrophic factor (BDNF) and enhance neurogenesis.
μ - opioid receptor: Radioligand binding experiments have confirmed that Tianeptin Sulfate has a partial excitatory effect on μ - opioid receptors (Ki ≈ 100 nM), but its affinity is lower than morphine (Ki ≈ 1 nM). Naloxone (opioid receptor antagonist) can partially block its antidepressant effect, indicating the involvement of μ - opioid receptors.
Dose conversion: There are differences between human clinical doses (12.5-25 mg/day) and rat equivalent doses (approximately 1-2 mg/kg/day), which may be related to inter species metabolic rates (such as hepatic enzyme activity) and receptor distribution density.
Sensitivity difference: Rodents are more sensitive to the activation of μ - opioid receptors, and low doses (5 mg/kg) can produce antidepressant effects, while humans require higher doses (25 mg/day) to observe similar effects.
Research on non-human primates (macaques): validation of bridge species
Behavioral Model
Social Separation Model
Macaque cubs exhibit anxiety like behaviors (such as curling up and increased self grooming) after social separation, and Tianeptine Sulfate (1-5 mg/kg, orally administered) can significantly alleviate these behaviors, with effects comparable to SSRIs (such as sertraline).
Cognitive task
Improve working memory task performance and suggest regulatory effects on prefrontal cortex function.
Neurobiological mechanisms
5-HT system
Microdialysis studies have shown that Tianeptin Sulfate (2 mg/kg) can enhance the reuptake of 5-HT in the prefrontal cortex and reduce the concentration of 5-HT in synaptic cleft, consistent with human and rodent studies.
Long term use upregulates 5-HT1A receptor expression and enhances receptor sensitivity.
Glutamate energy system
Inhibit glutamate release in the prefrontal cortex and reduce NMDA receptor activation.
Promote BDNF expression and enhance neural plasticity.
μ - opioid receptor
Radioligand binding experiments confirmed that Tianeptin Sulfate in macaque brain tissue has a similar affinity for μ - opioid receptors to humans (Ki ≈ 100 nM).
Naloxone can partially block its anti anxiety effect, indicating the involvement of μ - opioid receptors.
Comparison with Rodents
Behavioral consistency
Macaques and rodents exhibit similar antidepressant and anti anxiety behaviors, but macaques are closer to human social behavior and cognitive function.
Neurobiological conservation
The mechanisms of 5-HT, glutamatergy, and μ - opioid receptors in macaques are highly consistent with those in humans, confirming the preclinical value of rodent research.
Dose difference
The equivalent dose for macaques (1-5 mg/kg) is between that of humans (0.2-0.5 mg/kg, calculated based on body surface area) and rats (1-2 mg/kg), which may be related to metabolic rate and brain volume.
Consistency and specificity of cross species mechanisms
Consistency
Core mechanism conservation: Enhanced 5-HT reuptake, glutamatergic system regulation, and partial activation of μ - opioid receptors are common mechanisms of Tianeptin Sulfate Capsules in humans, rodents, and non-human primates.
Improvement of neuroplasticity: Long term use can promote neurogenesis and BDNF expression in the hippocampus/prefrontal cortex, which is associated with antidepressant efficacy.
Behavioral performance: The antidepressant, anti anxiety, and cognitive improvement effects are consistent across species, supporting their clinical application.
Dose effect difference: Rodents are more sensitive to the activation of μ - opioid receptors, and low doses can produce effects, while humans require higher doses.
Receptor distribution density: μ - opioid receptors are more densely distributed in rodent brain regions (such as the nucleus accumbens), which may explain their stronger regulatory effect on reward behavior.
Environmental adaptability: The social behavior and cognitive tasks of non-human primates (such as macaques) are more complex, and their drug responses may be closer to human clinical scenarios.
Drug interactions and special populations
In addition to serotonin syndrome, the combination of Tianeptin and MAOIs may also increase risks through other mechanisms:
Cardiovascular events: The combination of MAOIs and non-selective monoamine oxidase inhibitors may trigger paroxysmal hypertension, tachycardia, and even cardiogenic shock.
Anesthesia risk: Patients who have not discontinued Tianeptin before surgery may experience severe respiratory depression during the anesthesia induction period due to abnormally elevated 5-HT levels.
Taboos for special groups:
Elderly people: renal dysfunction leads to slow drug metabolism, making them prone to drug accumulation and poisoning;
Children: It is contraindicated for patients under 15 years old due to immature nervous system development, which makes them more sensitive to 5-HT fluctuations;
Individuals with renal insufficiency: The excretion of Tianeptin and its metabolites is reduced, significantly increasing the risk of poisoning.
Frequently Asked Questions
How strong is tianeptine compared to morphine?
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First, using a hot-plate analgesia test, the time point of maximal analgesic response was determined for tianeptine (15 min) and morphine (30 min), and then used for dose–response comparisons (Figure 2a). Tianeptine (ED50=15) showed a less potent analgesic response compared to morphine (ED50=3.1).
How does tianeptin affect the brain?
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In such models, tianeptine opposes the effects of chronic stress on brain structure and plasticity. For example, tianeptine prevented structural changes and modified neuronal metabolism and function in the hippocampus.
How long does it take for tianeptine to kick in?
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How long does it take for tianeptine to work? Users of online forums report tianeptine sodium and sulfate begins working within 30-60 minutes when taken orally. However, the onset of effects may be faster when taken via other routes of administration.
What is tianeptine sulfate used for?
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Tianeptine, sold under the brand names Stablon, Tatinol, and Coaxil among others, is an atypical tricyclic antidepressant which is used mainly in the treatment of major depressive disorder, although it may also be used to treat anxiety, asthma, and irritable bowel syndrome.
Is tianeptine good for anxiety?
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When taken in small doses, tianeptine may help with symptoms of anxiety, depression and irritable bowel syndrome. However, misuse can lead to taking larger doses and dependence. When taken at higher doses, tianeptine can cause a high or a feeling of euphoria. Taking high doses of tianeptine can be fatal.
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