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Tianeptine discovered to be MOR agonist

So, I gave tianeptine a rest for a few days, and then decided to take some this morning. When I filled a cap with about 100mg, I noticed there was only a bit left in the container, so I scooped it in totaling anywhere from 140-160mg. I balked for a second in the name of safety, but decided after everything I've read about people mega-dosing, as well as myself barely getting any effect from ~120mg, I didn't see any harm. I popped the cap about 1 hour after I took my daily kratom dose. One thing I remembered after the fact (foolish on my part) is that I took 600mg cimetidine 45 mins before I took my kratom. I think this may have had a strong potentiating effect on the tianeptine and I probably should have dosed less in hindsight.

By the time I arrived at work I found myself in a full-blown opiate daze. It wasn't just the coffee-like buzz I get from kratom, this was a much fuller, encapsulating, full body feeling more similar to a high dose of oxy/hydrocodone. Just the other day I plugged 40mg hydrocodone, which was a far more well-rounded opioid saturation, yet more subtle and ignorable. This, however, was nearly overwhelming in terms of peripheral effects, but the euphoria felt somewhat blunted though, as if there was more that could be had. What was being said above about the lack agonism on all opioid receptors makes perfect sense, that's how it felt. It was like kratom in a way, where it feels like it's hitting SOME opioid receptors, but not ALL of them like hydrocodone does....however the tianeptine definitely hit some receptors that kratom does not.

All in all it was a VERY enjoyable ~1.5-2 hours. The buzz slowly faded off and didn't leave me feeling like I needed to run home and lick the empty canister. Honestly, the high was pretty intense for an opioid high, I don't think I'd want to be any higher than that especially on an opioid RC.
 
Well if this is true then yeah, it would be useful for us who use opiates. However if it's anything like AH-7921 then it's virtually useless unless combined with another opioid. However it would help w/d as those Ruskis found out (and subsequently lost their arms).

With AH-7921 though (another selective MOR agonist), I found virtually no activity at the dose specified as it being active at. This made me question the entire philosophy behind opiates. I found it particularly effective though when used with other opioids. It would enhance them to the Nth degree, letting me use very, very small amounts of the opioid in question to achieve a high. For instance at that time I also had some MT-45 (which on it's own is active at around 80-100mg). I managed to use less than 10mg along with about 10mg of AH-7921 too along with some Chitosan just to help it absorb. I managed to finish a gram of each over about two weeks. Considering the duration of the high was about an hour or two, this is impressive.

Hence, I now believe the key to euphoria is either in d-agonism or just the potentiation of both m and d within the compound.

I still have a lot of Tianeptine, so I'll give this a go when I have more opioids. Though the rumour about it completely stopping working after a few months (whatever the dose) does worry me. I mean it could be playing havoc with your neurochemistry for all we know. It is the only reuptake enhancer known to man after all.
 
blueberries said:
It is the only reuptake enhancer known to man after all.
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Hasn't that been dis-proven? I could be wrong.

Something interesting with tianeptine, it seems to have stopped working altogether. The couple times I took ~150mg doses, I got a strong effect once, a moderate effect a couple times after, and now nothing whatsoever. I've taken breaks for up to a week and still, a 160mg dose produces absolutely no effects. I also do not notice it potentiating kratom at all. I did take hydrocodone one night long after I had already taken tianeptine (and kratom) and there's a chance that was a bit stronger, but there's no way to tell unless I do it again. With the under-studied nature of this drug, I'm going to shelf it for now and maybe bust it out again down the line.
 
The fact that it's a reuptake enhancer or that it's the only one??

If it's just the enhancer factor then I'm not too bothered. In all honesty it didn't fit into my mode of thinking anyway. If there's another RE though, I'd love to hear about it. Anyway if it were an MOR then it would be very light at that. Nothing compared to AH-7921 but then again it is an antidepressant analogue, therefore I'd expect it to have more affinity to neurotransmitters than opioid receptors like Amineptine does.

Having said that, could there be a possibility that it's just a straight SDRI with mild opioid agonistic properties? I haven't tried it concurrently with opioids but if you were getting only mild enhancement from a whopping 150mg dose (though tolerance is definitely in play here) then it can't be that potent as an opioid. Any opioid agonism, even delta, would give at least some increase in opioid affect, so this makes me think that it's opiate receptor affinity must be very light (though enough to keep the Russians giving an arm and a leg for it (!)).

I should try some more selective u agonists to test this theory, however there aren't too many on the market right now (mostly because alone they're crap). Having said that U-47700 should be a good one to try. Especially if I'm right. The price is next to nothing per hit and combined with opioids you could coast along for a month or two from a 100mg Morphine tab (especially with a bit of Chitosan in there).
 
Someone gave me a gram of this recently and I was impressed. I was taking huge doses to get the opiate effect for fun, but I was most impressed by the way it totally killed anxiety without any side effects (even at high doses like 150mg). One day I took 300mg spread out over 3-4 hours, and the anti-anxiety effect lasted way into the next day (seems like it wouldn't given it has such a short half life) and even a day after that. It has an effect that reminds me of SSRI's on emotions.. makes it impossible to get sad but at the same time kind of flattens out the happy stuff too.. only it does it instantly and with NO side effects.

Seems like it could be used as needed if you didn't want to take it daily... it seemed to work as good as xanax for anxiety without any sedation or other benzo effects. I can't think of any other non-benzo med that worked as good (other than things that fuck you up like alcohol or ghb etc).

Maybe it can be modified to extend the half life so only one dose a day is needed for anti-anxiety/depression.. or possibly it works just fine taking a bigger dose once a day.
 
yaesutom said:
.. or possibly it works just fine taking a bigger dose once a day.
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...or possibly you could take three (or more) doses spaced throughout the day as recommended
I don't see what makes you think a single large dose would be better for anything other than recreation. also tolerance
 
Decided to try a ~180mg dose on an empty stomach after a decent break, first thing in the morning (even before kratom) and observed no effects whatsoever. Strange stuff, as I was reading threads on people talking about shooting it and having a better effect than oxycodone and a slowly developing tolerance.
 
So to make a long story short, the tianeptine I first ordered worked like a charm, but ran out fast. I bought a second batch and it was missing it's silica pack, so it went bad really fast, which ironically was the same batch I wasn't getting effects from. So, on a third batch now, and a month long break, I tried 140mg. Perhaps some anxiety relief, and nothing else.

It seems like tolerance is sorta permanent with this stuff. Unfortunate, as stated above, it worked GREAT...when it worked.
 
I relatively recently purchased some tianeptine and gave it a try recreationally. I took anywhere from 40 to 150mg at once... the last few times I took 75mg doses, 3 of them spaces a couple of hours apart. I really found it to feel quite nice and I definitely saw a similarity to opiates. I was finding myself using it multiple days in a row and I caught myself after doing it probably 8 to 10 times total, because I quit a really destructive opiate habit of 10 years about a year ago. The next couple of days afterwards I felt slightly restless but no big deal. I gave the rest to my friends.

But yeah I did find it opiate-like, though certainly not nearly as strong. But enough to discontinue my use.
 
I take Tianeptine for a while now at therapeutic doses (i.e. 3x12,5mgs) and had high hopes for it, as i read many ppl seem to quite like it, mostly in doses up to 60-70mgs. As for me, in therapeutic dosing it turned out to be somewhat dull, even though i definitely feel it's Anti-Anxiety effects to a certain degree (nothing like Benzodiazepines effects of course) as well as being more confident. When dosing like i did, effects didn't appear instantly but within a few weeks, dunno remember exactly.
 
I just recently took somewhere between 175 and 225mg, and I can say that it feels really weird. Nothing like I've ever experienced before. To start off, my face is really itchy and I feel incredibly relaxed. My pupils are also very very tiny, which is strange since they're usually insanely dilated, without any particular reason. I do feel very happy, content, and almost a bit magical like you do on MDMA. There's definitely a body high. When I move around it feels weird, but really good. It feels like my arms and legs are filled with something magical, like water or some kind of energy. I don't necessarily have the urge to move, but it just feels really weird and nice at the same time.

This only really started a while after I started to feel the effects. In the beginning (like the first 30-60 minutes) it was just a jittery, slightly anxious but just more or less strange feeling. I continued to just browse the web like I was doing, and I soon noticed I was rubbing my face all the time. I then became more aware of the effects.

Since the notion of it being an SSRE seems to be disappearing, I'm curious how this combines with MDMA. It seems that if it is no longer classified as an SSRE it could potentiate its effects, like I remember some guy stating in his reports on Erowid. But I digress.
 
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Xorkoth said:
I relatively recently purchased some tianeptine and gave it a try recreationally. I took anywhere from 40 to 150mg at once... the last few times I took 75mg doses, 3 of them spaces a couple of hours apart. I really found it to feel quite nice and I definitely saw a similarity to opiates. I was finding myself using it multiple days in a row and I caught myself after doing it probably 8 to 10 times total, because I quit a really destructive opiate habit of 10 years about a year ago. The next couple of days afterwards I felt slightly restless but no big deal. I gave the rest to my friends.

But yeah I did find it opiate-like, though certainly not nearly as strong. But enough to discontinue my use.
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Good move, my friend. I bought it after my sub doc went MIA and I had no other opioid to turn to. Worked a charm. However, it didn't take long before I was up to 1g/dose, 3 doses a day. That's where I sit now' it didn't take long to get here, but tolerance hasn't gone up and I've been sitting at this dose for a couple months now. I know the numbers say it's way weaker than morphine, but I've found it to be more like 1/3 the potency of oxy- as in 300mg is roughly equal to 100mg of oxy. Well, between 70 and 100. After taking 300mg 3 x daily, I tried getting high with oxy, and 70mg was barely perceptible, it took snorting another 30mg to get to the same place 300mg of Tianeptine would have had me.
 
I believe there's a big difference in oral dose 150 mg tianeptine and even just 70 mg's I.v. Speaking from some long term opiod/opiate tolerance. I think skipping the first pass metabolism (the liver) may play a part in the difference. It's true any I.v. medication will eventually go back to the liver, but this happens after that drug is metabolized. I'm not just referring to an increase in BOA but a different action of metabolism because the primary metabolism of tiaenpt. is listed as hepatic.
 
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