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how potent of an opiate is tianeptine, really??

@allone

Believe me when I say that Tianeptine is highly overrated

What you do yourself with it is up to you

Yeah, some cats inject it and claim it's just as strong as heroin....

I also think those people are fucking fools

Tried it, assessed it.... it's fucking shit and overrated

But there will always be those people who inject stupid amounts and claim its better than heroin.... fools in my opinion or unique body chemistry

There is a reason it's unscheduled..... a very good reason... it's not that great
 
allone said:
It seems there is HUGE underestimate of the power of this stuff as a super potent opiate. this is coming after few months of use on and off, then going through a car crash, and being stuck in the hospital without being able to use it, instead stuck with 6 time doses of morphine a day without any effect at all!!
Yes, i already have prior tolerance to suboxone, which is a bitch, but i havent been using suboxone for at least 2 weeks prior to the accident, with only high dose tianeptine daily, 2 times a day or once a night as needed. Then ending up with both morphine AND tramadol combo not enough to even compare to tianeptine!
i was going through an actual opiate withdrawal while on 250mg tramadol in fact. I had to switch back to suboxone, as that was my main drug of use before all shit happened, and guess what? AGAIN, no fucking effect at really high dose, 12mg or more a day. WTF is going on, and whats the deal with tianeptine?? Is this the most potent underrated opiate to date, or what?? Tell you what, it probably is, and it is the most underdiscussed underrrated opiate in the existence that is still in fact LEGAL!!
My god this stuff is so dangerious. It needs to be off the market, QUICK. please help me ban it!

BTW I just ordered more! I couldnt take this shit anymore, sorry for this. I know I want to ban it, but I cant help but have more meanwhile..... :S:SS:S
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It's pretty weak. For affinity, it is around Ki 450 nMol. But affinity in vitro and potency in vivo do not always translate. For instance, bupropion is a very weak DRI with an affinity around 500 nMol and a half maximum inhibitory potency of 6.5 Umol. That is very weak, but BP does inhibit somewhat dopamine reuptake in vivo, especially at doses above 400 mg.

Tianeptine is abusable, but most cases of abuse have involved intravenous injection of high doses. Taken orally, the doses needed for psychological dependence are much higher than doses used for depression. Morphine, the prototypical Mu opioid ligand, is about 100 X more potent. But tianeptine is a very risky antidepressant for people with a history of drug depence. Another antidepressant like that is the antidepressant amineptine, a chemical cousin of tianeptine, a potent DRI almost 10 X more potent than bupropion for inhibiting the reuptake of dopamine. Amineptine has actually been abused much more than tianeptine which led it to be removed from the global markets. It is also a potent substrate for CYP3A4, and is the most hepatotoxic of all tricyclics. The abuse potential and hepatotoxicity, with many cases of liver damage, led to it being removed from the global markets. It shows cross-tolerance with both amphetamine and cocaine.
 
I’m curious what the effect of Tianeptine while on 12 mgs of suboxone? After reading how bad it can be I’d rather go back to shooting h.
 
Bravoncius Roxford said:
It's pretty weak. For affinity, it is around Ki 450 nMol. But affinity in vitro and potency in vivo do not always translate. For instance, bupropion is a very weak DRI with an affinity around 500 nMol and a half maximum inhibitory potency of 6.5 Umol. That is very weak, but BP does inhibit somewhat dopamine reuptake in vivo, especially at doses above 400 mg.

Tianeptine is abusable, but most cases of abuse have involved intravenous injection of high doses. Taken orally, the doses needed for psychological dependence are much higher than doses used for depression. Morphine, the prototypical Mu opioid ligand, is about 100 X more potent. But tianeptine is a very risky antidepressant for people with a history of drug depence. Another antidepressant like that is the antidepressant amineptine, a chemical cousin of tianeptine, a potent DRI almost 10 X more potent than bupropion for inhibiting the reuptake of dopamine. Amineptine has actually been abused much more than tianeptine which led it to be removed from the global markets. It is also a potent substrate for CYP3A4, and is the most hepatotoxic of all tricyclics. The abuse potential and hepatotoxicity, with many cases of liver damage, led to it being removed from the global markets. It shows cross-tolerance with both amphetamine and cocaine.
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I thought it was closer to 350nM with an IC50 of 200 or so.

In practice it is a pretty high efficacy MOR agonist, though not a particularly potent one.

From my extensive experience with it I would roughly equate tianeptine as being 1/10th the potency of morphine despite have Ki value 200x greater. Some of the better batches felt like 1/8th the potency of morphine.

I really enjoyed it for a while but got sick of it and/or the synthesis quality dropped significantly. In its sodium form it is quite fast acting and has a pronounced rush.
 
Absoluteolive said:
I’m curious what the effect of Tianeptine while on 12 mgs of suboxone? After reading how bad it can be I’d rather go back to shooting h.
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ive been doing suboxone for a long time and tianeptine is the only shit that really actually takes subs away from use, or works in actual synchronicity, which is crazy but true in my case.

negrogesic, tianeptine for me was stronger than morphine when i was in a car crash. i went to the hospital, severe MF pain! they shoot me with morphine every few hours and i dont feel shit. Then my mom brought me tianeptine illegally in a sock and i just had 2 small tea spoons a day and shit, ALL PAIN GONE. to this day i do not get it. perhaps it works synergistic with morphine?? maybe....
 
allone said:
ive been doing suboxone for a long time and tianeptine is the only shit that really actually takes subs away from use, or works in actual synchronicity, which is crazy but true in my case.

negrogesic, tianeptine for me was stronger than morphine when i was in a car crash. i went to the hospital, severe MF pain! they shoot me with morphine every few hours and i dont feel shit. Then my mom brought me tianeptine illegally in a sock and i just had 2 small tea spoons a day and shit, ALL PAIN GONE. to this day i do not get it. perhaps it works synergistic with morphine?? maybe....
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Interesting. You can feel tianeptine through the suboxone? How much tianeptine do you need to feel it through the suboxone?

FYI, two teaspons would be a very large dose of tianeptine, amounting to multiple grams. That would definitely be very effective in relieving pain. Also very effective in starting a tianeptine addiction.

Ive heard of people using 10g a day of tianeptine, so much so that methadone or a shot of heroin doesnt relieve their pain.

The highest I ever got was 1.5g a day. A single dose of 1.5g had me high for a good 20 hours. I miss the old tianeptine but these modern batches suck in comparison. What they lack in high they make up for in nausea and side-effects.
 
well, new tianeptine batch is coming for me to try and ill see if its any good. and yes, i felt it through suboxone. of course, the high is limited if you have been on suboxone for a while because of opiate tolerance and all that bullshit, but im saying suboxone doesnt really stop or interfere, completely at least. but because of the tolerance, thanks to the damn suboxone, the high isnt as magical as it used to be when i was off opiates for few months, duh!
im thinking of using clonidine now to counteract the nasty burn out feeling afterwards. any ideas about such a mix? i already tried clonidine before without feeling shit. ill just bump the dose and see if it calms my ass down when tianeptine overstimulates it!
 
Not sure about how clonidine fits in here, but as far as the stimulating effects of tianeptine, what ive notice is that inspite of its stimulating effects, if i were to take say a gram in the morning, that night i would sleep incredibly well. If i were to take it 4 hours before bed however I'd be up all night. Sleeping during the tail end of a tianeptine sodium high is amazing.
 
"Sleeping during the tail end of a tianeptine sodium high is amazing" yeah ive noticed too but i wonder if its just burn n crash type of situation. i would dose a lot during the day, by night or usually morning, ill be dead in bed and sleep like 12 hours. suboxone does kind of the same thing to me. they seem to affect the adrenal gland somehow pretty heavy i suppose
 
schizopath said:
I always thought of tianeptine as the ultimate "this will totally fuck all of your receptors up" kind of substance. Might be wrong but still be Careful 🖤
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fuck em all up, how? it has serious glutamate action which can be quite uncomfortable weird effect long term and it is said it might help with addictions, kind of like ketamine might work too. i personally find less interest in abusing drugs or alcohol after a binge of tianeptine for a week or so. of course it all goes back to prior eventually. how do you assume it might fuck em permanently though? i mean it did make me hate a lot of things i used to enjoy before without using it but it could also just be its potent opiate activity and association with activities which arent enjoyable without it anymore. even if it did mess up your receptors, could it be really serious long term irreversible??
 
russian antidepressant?? its french. made in the 60s by the french society of medical research (that sounds pretty fancy and high class right there btw)

but my biggest problem with it now is, after reading some articles, its hepatoxicity! so a similar chemical was made before it and proved to be very hepatoxic so it was dropped in favor of this one. BUT it never mentions this one is much safer, and there are actually articles mentioning its liver toxicity, which worries me!
I would love if someone with more knowledge in biochemistry check some of those liver toxicity articles and report back of how serious they might be, please, thanks!!!
 
A New York City Professor had done a patent on this subject.

To get the optimal potency for the mu-opioid receptor,

change the chlorine halogen in tianeptine for fluorine, and the ethyl ester is left unsaponified for the last step.

You can find it in the database yourself or i can show you it.
 
Smyth2 said:
A New York City Professor had done a patent on this subject.

To get the optimal potency for the mu-opioid receptor,

change the chlorine halogen in tianeptine for fluorine, and the ethyl ester is left unsaponified for the last step.

You can find it in the database yourself or i can show you it.
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I tried ethyl tianeptine I, or i suppose what you'd call ethyliododeschlorotianeptine and it was about 5 times stronger of a mu-agonist. Also very caustic. Having a slower onset however made it less recreational than tianeptine sodium.
 
hmm interesting why they dont sell this variant. they have sulfate (which sucks) and acid, which i dunno much about. but i have never heard of this one until now!
negrogesic, how the hell did you get a hold of such a rare substance anyhow wow
 
btw i got my tianeptine and i used clonidine to take off the edge and it works. there was a person complaining here about long term edge feeling after initial high, but clonidine seems to do the work. or simply drink beer? or benzos? there are choices out there.
anyway, i have been on suboxone for a while and the major euphoria does seem to be a bit subdued, kind of not the same at all. negrogesic im afraid both of us might have reached our initial euphoric moment with this one and now we are kind of adapted which sucks. I do believe though, 1-2 months total absence of opiates, and you will get a super high from this shit, especially one i get.
 
allone said:
btw i got my tianeptine and i used clonidine to take off the edge and it works. there was a person complaining here about long term edge feeling after initial high, but clonidine seems to do the work. or simply drink beer? or benzos? there are choices out there.
anyway, i have been on suboxone for a while and the major euphoria does seem to be a bit subdued, kind of not the same at all. negrogesic im afraid both of us might have reached our initial euphoric moment with this one and now we are kind of adapted which sucks. I do believe though, 1-2 months total absence of opiates, and you will get a super high from this shit, especially one i get.
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How many mgs of suboxone are you on? Curious I’m on 12. Started at 24 a year me a half ago..
 
allone said:
what? is it illegal in ireland to just simply order it online? actually, i believe it is not because nobody even knows what that shit is over there. you can always just get it prescribed as Coaxil for depression there since its Europe.
But anyway, what type of research are you going to do with it? and from which source did you order, can you please tell me?
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I’m only seeing this, when you don’t use the reply I don’t get a notification.

It is legal for me to get but I do work in a lab. I also can’t name my sources here. It’s against the BLUA as well as professionally it wouldn’t be very wise.

Honestly and I’ve seen you mention it on down, the hepatotoxicity is very interesting to me and I thought it would be a good study for part of my PhD tbh. Not sure what angle I’ll come at it yet to be honest but...

Here is part of a paper... I’ll post the link at the bottom.


Tianeptine--an instance of drug-induced hepatotoxicity predicted by prospective experimental studies.​

Abstract​


We report the case of a patient who developed acute hepatitis after taking tianeptine, a new tricyclic antidepressant, for 8 weeks. Hepatitis exhibited cholangitis-like clinical features and was associated with hypersensitivity manifestations suggestive of an immuno-allergic mechanism. Histological examination showed microvesicular steatosis. The discontinuation of tianeptine administration was followed by complete recovery. Immunoallergic hepatitis and microvesicular steatosis were predicted 2 years ago from prospective experimental studies prompted by the similarity of the chemical structures of tianeptine and amineptine, another tricyclic antidepressant, well-known for its hepatotoxicity. Experimentally, tianeptine has been found to be oxidized into reactive metabolites in several rodents and human liver and to produce microvesicular steatosis probably through inhibition of mitochondrial beta-oxidation of fatty acid in mice. This case illustrates the value of prospectively assessing potential hepatotoxicity mechanisms for new compounds chemically related to drugs already known to be hepatotoxic.

 
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