Why You Should Choose Us As Your Tianeptine Supplier?
#1. High quality with the best price:
Our standards are EP9.0 and you will get the best price you can ever find in the market.
#2. Quality guarantee:
100% refund for any quality issues after testing.
#3. Fast shipment:
Goods will be shipped out after rapid repacking and a tracking number will be provided to you within 3~4 days.
#4. Steady supply:
We keep kilos in stock for prompt shipment.
Repacking can be arranged within 1 working day!
What Is Tianeptine Sodium?
Cas number: 30123-17-2
Molecular Formula: C21H24ClN2NaO4S
Molecular Weight: 458.9 g/mol
HS Code: 2934991000
Tianeptine sodium is a white to yellowish and very hygroscopic powder.
When its purity is over 99%, it tends to be snow-white rather than yellowish.
As it is strongly prone to absorb moisture in the air, it should be sealed and stored properly before they become rocks after leeching water.
The color difference is partially caused by water content inside or by impurity.
What Is Tianeptine Sodium Used For?
Tianeptine Na has been used as an atypical antidepressant for the treatment of major depressive disorders.
It is also used to treat anxiety, asthma, and irritable bowel syndrome.
Sodium Tianeptine is marketed as Stablon and Coaxil in many countries for depression.
People also use it for treating pain caused by fibromyalgia because of its anticonvulsant and analgesic effects.
It has been effective in the treatment of attention-deficit hyperactivity disorder with minimal side effects too.
How Is Tianeptine Sodium Produced?
Sodium tianeptine is produced by a 3-step synthesis route: condensation, hydrolysis, salt formation.
Flow-chart is as below:
Some of you would argue that they only see 2 steps.
While you can see that the condensation and hydrolysis are completed in the same step.
Later the acid is turned into sodium salt and got spray-dried into the end product: sodium salt.
We will break it down step by step.
#Step1: Condensation
Preparation of ethyl 7-[(3-chloro-6,11-dihydro-5,5-dioxo-6-methyl-dibenzo[C,f][1,2]thiazol-11yl)amino]heptanoate.
We use 3,11-dichloro-6,11-dihydro-6-methyl-dibenzo[c,f] [1,2]thiazepine-5,5-dioxide as starting material, condensed with ethyl 7-aminoheptanoate hydrochloride.
The molar ratio of the two is 1:(1.0-1.25), add 5 times the amount of acetonitrile as solvent.
Stir well, and then add 1:(2.0-2.25) equivalents of Triethylamine.
Heat it to 50°C -60°C and keep the reaction going for 2 hours and then concentrate it dry under reduced pressure.
Add dichloromethane, water, then stir the mixture for 0.5 hours.
Stand partition, take the organic layer, then wash it with water.
Then combine both organic phases, concentrate them under reduced pressure to obtain reddish-brown, viscous 7-[(3-chloro-6,11- dihydro-5,5-dioxo-6-methyldibenzo[c,f](1,2)thiazol-11yl)amino] Ethyl heptanoate.
This step has an 81%-yield, with 98.5% as purity.
#Step 2: Hydrolysis
Synthesis of 7-[(3-chloro-6,11-dihydro-5,5-dioxo-6-methyl-dibenzo[C,f][1,2]thiazole-11
(3-chloro-6,11-dihydro-5,5-dioxo-6-methyl-dibenzo[C,f][1,2]thiazole-11)amino]heptanoic acid, also known as the preparation of tianeptine free acid.
Add 1.31 mol of the red-brown, viscous material above to an ethanol&10% aqueous sodium hydroxide solution.
Adjust and keep the reaction solution PH no less than 8.
Heat up the temperature to 50-60°C, and let it react for 30 minutes.
At the same time, keep checking the PH of the reaction solution.
If it is lower than 8, it is necessary to add the alkali solution to ensure the PH of the system PH=8-9.
After the reaction, evaporate the ethanol under reduced pressure to obtain the viscous residue.
Add deionized water, dichloromethane.
Stir, and use concentrated hydrochloric acid to adjust until the material is well layered out.
Separate the organic phase, extract the aqueous phase with dichloromethane.
Then combine the organic phase and concentrate to dryness.
Add anhydrous ethanol, dissolve by heating, lower the temperature to 5°C and stir the crystals for 2 hours, filter,
The filter cake was dried under vacuum at 50-60°C for 20-24 hours, and then the crude white powder of tianeptine was obtained.
The crude product is heated in ethanol and dissolved again.
Then we cool it to get crystals.
Later crystals are filtered and dried to obtain 7_[(3_gas-6,11-dioxo-5,5_dioxo_6_methyldibenzo[c,f][1,2]thiazol-11yl)amino]heptanoic acid white powder, with an 80% yield and 99.5% pure.
#Step3: Preparation of sodium salt.
Take 0.9 mol of tianeptine free acid into the reaction kettle, then add deionized water, stir it well.
And then heat it to 45°C till the material is in suspension.
Put 15% aqueous sodium hydroxide solution into the reaction kettle.
Drop it within 30min, and make sure to keep the internal temperature 38°C-45°C.
After stirring it for 30 minutes, add to the activated carbon and heat it to 55°C~60°C.
Continue stirring for 2 hours.
The filtrate is filtered through a 0.45-micron pore size membrane, and the filtrate is brought to room temperature and spray dried directly to salt using a spray dryer.
The end product was obtained as a white-powder tianeptine sodium 330g, with a yield of 82.5% and purity of 99.7%.
Is Tianeptine Sodium A Nootropic?
The answer is Yes.
Nootropics, also known as smart drugs, are used to improve cognitive function, particularly executive functions, memory, creativity, or motivation in healthy individuals.
Tianeptine is a TCA-like and serotonergic enhancing medication prescribed commonly in the Middle East and Europe for depression and anxiety.
However, the study shows it does help to improve people’s cognitive functions.
The FDA has not approved Tianeptine for any use in the United States for any conditions, let alone allow it to be used to improve cognitive functions.
Tianeptine Sodium vs Sulfate
There are three commonly seen Tianeptine forms on the market: Tianeptine free acid, sodium salt, and tianeptine sulfate salt.
Among them, tianeptine acid is the least popular and cheapest type.
Maybe tianeptine free acid only exists because it can be made into various tianeptine salts such as tianeptine hydrochloride, tianeptine tosylate, tianeptine phosphate, etc.
So here we only list the difference between tianeptine sodium and tianeptine sulfate (also written as tianeptine sulfate).
1. Their age. (Sodium is older than sulfate)
Sodium tianeptine is the first to be widely used for medical purposes for depression since 1960.
Tianeptine sulfate is later developed and improved versions to replace the sodium form.
2. Stability. (sulfate salt is more stable than sodium salt)
Both tianeptine sodium and sulfate are stable when protected from light and air.
But sodium salt is very hygroscopic to get chunky.
While tianeptine sulfate salt contains monohydrate with itself, it is more stable when exposed to air for a short period.
3. Water solubility uniformity. (Tianeptine sulfate has better uniformity than sodium)
In water solutions PH ranged 1~6, the soluble amount of tianeptine sulfate in water is very average.
Its solubility curve is very smooth, the value gets slightly smaller as the PH goes up.
While sodium salt has a sudden drop when PH goes from 1 to 6.
As the stomach fluid PH ranges from 1.5~3.5 and sure you will choose sulfate to maintain a stable solubility.
4. Taste. (Tianeptine sulfate is not bitter, sodium is)
The bitterness of sodium tianeptine can linger in your mouth for one month if it is taken directly.
While tianeptine sulfate is much better on the taste, no such strong bitterness at all.
That’s why you only see tianeptine sodium capsules but rarely see any tianeptine sodium tablets on the market.
5. Half-life and Bioavailability. (Tianeptine sulfate lasts longer than sodium)
According to researches and online reviews, tianeptine sulfate performs better on both half-life and bioavailability.
Sulfate is easier to absorb and its effect lasts longer, while dosing sodium can go 6~7 times daily to obtain the same effect as sulfate.
6. Price. (Tianeptine Sulfate is 20% higher than sodium)
As tianeptine sulfate has better performance almost on any aspect than tianeptine sodium and the production process is a little more complicated, its price is also a little higher, which does make sense.
Tianeptine vs Trazodone
Both Trazodone HCl and Tianeptine can be used for the treatment of depression.
What are their differences?
#1. Different Indications.
Tianeptine sodium is mainly used for the treatment of classic depressive episodes.
Trazodone is a tetracyclic atypical antidepressant that selectively antagonizes 5-hydroxytryptamine (5-HT) reuptake and weakly blocks norepinephrine (NA) reuptake, but has no effect on dopamine (DA), histamine, or acetylcholine.
It will not inhibit the activity of monoamine oxidase inhibitors (MAO) in the brain.
In addition, trazodone has antagonistic effects on 5-HT2A receptors or 5-HT2C receptors.
Trazadone can effectively improve sleeping issues, such as it will significantly shorten the sleep latency of depressed patients, prolong the overall sleep time and improve their sleep qualities.
#2. Approval date and Range
Trazodone has been approved for medical use in the United States in 1981. It is used more widely.
It was approved in the Netherlands in 2014 in form of 100mg tablets.
While Tianeptine has not been authorized by USFDA for any indications in the United States until today.
Though tianeptine is approved and marketed in many European countries, the UK has not approved it yet for depression yet.
#3. Cost differences
The price for Trazodone as a bulk ingredient is much lower.
The cost of trazodone is about 1/7 of that of Tianeptine.
Trazodone costs about 600~800USD/kilo, while the price for tianeptine per kilo is around 3000USD.
What are Tianeptine Sodium’s Side Effects?
#1. Common side effects(>1% frequency)
Headache (up to 18%) / Dizziness (up to 10%) / Insomnia/nightmares (up to 20%) / Drowsiness (up to 10%) / Dry mouth (up to 20%) / Constipation (up to 15%) / Nausea / Abdominal pain / Weight gain (~3%) / Agitation / Anxiety / irritability
#2. Uncommon side effects(0.1-1% frequency)
Bitter taste / Flatulence / Gastralgia / Blurred vision / Muscle aches / Premature ventricular contractions / Micturition disturbances / Palpitations / Orthostatic hypotension / Hot flushes / Tremor Rare (<0.1% frequency) / Hepatitis / Hypomania / Euphoria / ECG changes / Pruritus / allergic-type / skin reactions / Protracted muscle aches
Warnings (tianeptine sodium withdrawal)
According to tianeptine marketer Servier, stopping treatment with tianeptine is difficult, due to the possibility of withdrawal symptoms in a person.
The severity of the tianeptine withdrawal is dependent on the daily dose, with high doses being extremely difficult to quit.
DEA states that the withdrawal symptoms in humans typically result in agitation, nausea, vomiting, tachycardia, hypertension, diarrhea, tremor, and diaphoresis.
Data are demonstrating that the abuse of tianeptine is increasing while contributing to the current opioid epidemic.
How Much Does Tianeptine Sodium Powder Cost?
Currently, we have it for sale and our running stock is 25kg to keep it always fresh.
The price from us for commercial order quantities of 50kg or more is around 2900USD/kg.
For quantities of 10kg, our cost is around 3000USD/KG.
If you only buy 1kilo, our price is about 3300USD/KG.
For costs of 100Gram, our offer is about 550USD including shipping.
As all prices are subject to raw material price fluctuations, please contact us directly for more accurate prices.
For a better comparison, you check prices below from other online stores for your ref.
Price from tianeptinedirect is 6500usd per kilo
Tianeptinebuyonline is selling by 800usd per 100g
Price from tianeptinestore is 440usd per 50g
Cost from savant-research is 106usd per 10g
Where To Buy Tianeptine Locally?
As you can see from the prices from other suppliers above, their unit prices for 1kilo is over 7000USD as the wholesale price.
#1. If you are close to them and need them urgently, and you are willing to pay some extra dollars, so shipping from your local vendors means there is no need for your chemicals to pass borders.
And you can choose them with lower MOQ to 10 Grams and Higher prices.
#2. If you are a buyer from another country other than the sellers are located, and they will not ship the goods from your local warehouses.
Please contact us now for a quick order, we will manage to get you the best prices.
Currently, we have 27.5 Kilo as Running Stock Ready For Fast Shipping.
You can check our terms below and prices from other suppliers above for your decision.
How To Ship and Store Tianeptine Sodium?
Firstly, let’s talk about the shipping options.
Tianeptine sodium is a safe chemical to be shipped by air or courier.
It is not dangerous or bio-poisonous, with RAT ORAL LD50 as over 1100mg/kilo.
It is not flammable or explosive, it can bear small bumps.
We’ve also gotten its certificate of safe air transportation from DGM, SRICI, etc, which is firm proof for its safety as a common chemical.
If it is safe to be shipped by air or express, shipping by sea and rail won’t be a problem at all.
Secondly: For the storage and shipping conditions, we will break them one by one.
We have run stability tests for its storage, both at accelerated or common room temperature conditions.
The stability testing results have shown that sodium salt is stable for at least 24 months under room temperature, on the condition of proper sealing and protection from the sunlight.
Though it is stable for 2 years by room temperature, it does not mean it will not go bad during transportation.
You have to make sure that the cabin temperature is not too high and the goods are properly sealed and protected from light.
As a result, during your storage, you need to seal it well to protect it from possible moisture or light during transportation.
When it has reached your warehouse, store it in a cool, dry, and temperature-stable environment.
Technical Documents Download
References
- Tianeptine in wikipedia
- Tianeptine In Pubchem
- https://www.drugbank.ca/salts/DBSALT001784
- https://patents.google.com/patent/US8198268B2/en
- https://www.quora.com/Whats-it-like-to-take-Tianeptine-sulfate
- Trazodone in wikipedia
