Tianeptine’s Action At Opioid Receptors, Kis Vales Provided

[muie]

There are many experts amongst our members who know a lot more about receptor affinity than I and many others. I've posted a chart showing the Kis values.

Could someone more experienced place tianeptine in terms of strength/receptor affinity, between the opioids/opiates with the most similar Kis values?
For example: from these numbers alone, would you place it between tramadol & codeine or between hydrocodone & demerol?

The following chart summarizes tianeptine's activity at the opioid receptors! The article, tested it on virtually all receptors including benzodiazepine, cannabinoid, serotonin, dopamine, etc, and only the opioid receptors showed any activity, minus the K-opioid receptor which was also found inactive.

Its worth a read! The full article is here:
http://www.nature.com/tp/journal/v4/n7/full/tp201430a.html

"Summary of tianeptine’s activity at the opioid receptors. (a) Chemical structure of tianeptine. (b) Radioligand displacement binding assay of tianeptine at μ-opioid receptor (MOR; n=3), δ-opioid receptor (DOR; n=4) and κ-opioid receptor (KOR; n=4). Tianeptine’s functional activity at MOR, DOR and KOR are also summarized. Data represent mean±s.e.m."

Figure 1.
http://www.nature.com/tp/journal/v4/n7/fig_tab/tp201430f1.html#figure-title

p.s. There is a very important reason why research testing on mice & rats, while mammals, shouldn't be used as a definitive guide to predict effects on humans! The following quote, taken from this article is a case in point:

"Interestingly, we also found a difference in the potency of tianeptine between the human and mouse DOR; in this case, tianeptine was less potent at the hDOR (EC50 (hDOR, G protein)=37.4±11.2 μM). Thus, while the selectivity of MOR over DOR is approximately 20-fold in mouse, it is nearly 200-fold in human."

 

[Prescottdave]

" The following chart summarizes tianeptine's activity at the opioid receptors! The article, tested it on virtually all receptors including benzodiazepine, cannabinoid, serotonin, dopamine, etc, and only the opioid receptors showed any activity, minus the K-opioid receptor which was also found inactive."
Very interesting. Thanks for the info. So from what I can gather from this specific source is that tianeptine does not directly or indirectly affect dopamine or serotonin?

 

[kleinerkiffer]

Od -> N&PD

 

[asecin]

umm confusion here. i thought there are quite a bit of papers demonstrating its activity at serotonin for definitive but also other areas with some low inhibition of dopamine?

 

[serotonin2A]

umm confusion here. i thought there are quite a bit of papers demonstrating its activity at serotonin for definitive but also other areas with some low inhibition of dopamine?

Most of the characterization was performed prior to the a development of many modern pharmacological techniques. It needs to be re-characterized to understand how it works. It has opioid effects but the doses required to induce those effects on vivo are supra-therapeutic. Much work is also needed to determine exactly how it interacts with MOR.

 

[Zeds(NCO2CH2CH3)2]

At the end of the day I'm predicting Tianeptine binds to mOR as a biased agonist and also inhibits CCK, in parallel. In high doses we can see the reward in that maybe. Further evaluation of the assay papers assay conditions would tell morw

 

[JohnBoy2000]

Is tianeptine available int the US?

I've been looking at this myself due to it's opioid agonist properties, and lack of nasty anticholinergic side effects.
Seems to stand alone in the AD catagory in terms of this effect.
Other AD's seem to be more "downstream" in terms of their opioid implications.

Has anyone actually tried tianeptine?

 

[SKL]

Many people have, including many on BL including myself. I liked it when I first tried it nut found it useless once I had a serious opiate tolerance. Unfortunately it's quite readily available by shady online vendors, but is not an approved prescription drug in the U.S. I'd be very wary of it as lots of unpleasantness is surfacing regarding long term high dose use etc.

 

[Tryptamite]

It will hold off WDs even from a relatively high dose habit with supra therapeutic doses IV. I do not know if the same or slightly higher dose oral will work as well.
But 300mg IV was certainly noticeable on about 60mg methadone a day and kept me well for a few hours.
I would rank it above tramadol, codeine, dihydrocodeine. Subjectively even though I only tried oxycodone years after I would say I prefer it to oxycodone.

It is hard on the veins though.

 

[asecin]

ok why are you guys concentrating on its stupid opiate effects, im more curious of what other things influences besides the side effect opioid feel

 

[Tryptamite]

I would like to know to.

 

[asecin]

yeh its opioid effects are such a turn off. and its antidepressant, must be some else at work here. if anything opoiods are depressants

 

[belligerent drunk]

^ opioids, acutely, act as antidepressants.