DXM+serotonin reabsorbtion enhancer

[Renald]

Lets discuss can taking of DXM with SSRE remove its serotonergic action? I have read tianeptine is thought being an SSRE.

 

[Kaleida]

To what end? If you're trying to make it safe to mix with MDMA or something, I promise there are far better and safer options to explore, like just using a different dissociative.

To my knowledge, there is currently no such known thing as a selective serotonin reuptake enhancer. The original assumptions about tianeptine were wrong; it is now known to be an opioid that does not alter serotonin reuptake.

 

[HeadHigh]

Kaleida, please reference from what source you found this information about tianeptine. I would be very interested in reading about that since i have not seen it anywhere

 

[Kaleida]

Here are a few:

Effects of acute and chronic tianeptine administration on serotonin outflow in rats: comparison with paroxetine by using in vivo microdialysis.

...A single paroxetine dose (1 mg/kg, i.p.) increased [5-HT]_ext over baseline in the frontal cortex and raphe nuclei, respectively. A single administration of tianeptine (10 mg/kg, i.p.) did not change [5-HT_ext] in the two brain regions studied. Repeated exposure to paroxetine (0.5 mg/kg) b.i.d. for 14 days induced a sixfold significant increase in basal [5-HT]_ext in the raphe nuclei. Administration of tianeptine (5 mg/kg) b.i.d. for 14 days did not affect 5-HT baseline concentrations. In rats chronically treated with either paroxetine or tianeptine, drug challenge did not alter area under the curve values. Thus, our in vivo data indicate that tianeptine and paroxetine do not exert a similar in vivo effect on the serotonergic system in rat brain.

Effect of acute and prolonged tianeptine administration on the 5-HT transporter: electrophysiological, biochemical and radioligand binding studies in the rat brain.

...Microiontophoretic application of tianeptine onto dorsal hippocampus CA₃ pyramidal neurons, as well as its intravenous administration (2 mg/kg), increased their firing frequency. Following intracerebroventricular administration of 5,7-dihydroxytryptamine, the activation induced by the microiontophoretic application of tianeptine remained unchanged, thus suggesting that the 5-HT carrier is not involved in this effect. Furthermore, in spite of its activating effect on CA₃ pyramidal neuron firing frequency, the intravenous administration of tianeptine did not alter the time of recovery of these neurons from microiontophoretic applications of 5-HT, an index of 5-HT uptake activity. In keeping with this observation, the acute administration of tianeptine did not change the effectiveness of the 5-HT reuptake blocker paroxetine (1 mg/kg, i.v.) in prolonging the suppressant effect of microiontophoretically-applied 5-HT.

...The effectiveness of paroxetine to block [³H]5-HT uptake was unchanged in slices obtained from rats still bearing the osmotic minipump at the time of the sacrifice, as well as from those which had undergone a 48 h washout period. To assess whether prolonged administration of tianeptine would induce adaptive changes on 5-HT uptake sites, [³H]cyanoimipramine-binding parameters were measured following a 48 h washout period. Affinity values remained unchanged while density values were significantly increased in cortex (+22%) but not in hippocampus (+12%). It is concluded that, i) the activation of CA₃ pyramidal neurons observed following acute tianeptine administration cannot be attributed to its 5-HT uptake enhancing properties and ii) the prolonged administration of tianeptine induces adaptive changes on cortical but not on hippocampal 5-HT transporters.

Tianeptine treatment induces regionally specific changes in monoamine.

...Few changes were noted in the 5-HT system. 5-HT levels were increased by short-term tianeptine in the CA3 region of hippocampus, and 5-hydroxyindoleacetic acid (5-HIAA) was increased in the ventromedial nucleus of hypothalamus, while 5-HT turnover was decreased in preoptic area (POA).

These studies are actually fifteen to twenty years old at this point, and the original one suggesting that tianeptine could be a serotonin reuptake enhancer is from 1987. It really hasn't been a valid theory for quite some time now.

 

[Renald]

It is more a theoretical discussion, I am interested in how would DXM feel without a serotonergic action. Will it be like a typical dissociative, ketamine like? Also, it would be interesting to block its sigma action and look what happens.

 

[HeadHigh]

Thank you Kaleida, that was very insightful for my research on this drug.

In my opinion Renald, Tianeptine would most likely add more to the physical effects of DXM because of its action on the opioid receptors, and would most likely not dampen the serotonergic effects at all

 

[Sprout]

It is more a theoretical discussion, I am interested in how would DXM feel without a serotonergic action. Will it be like a typical dissociative, ketamine like? Also, it would be interesting to block its sigma action and look what happens.

Its metabolism to the opioidergic product would still occur, it's just a filthy drug pharmacologically.

 

[LucidSDreamr]

Its metabolism to the opioidergic product would still occur, it's just a filthy drug pharmacologically.

agreed but it has still mange to repeatedly product euphoria shitting on mdma...holes and CEVs that rival IV mxe, and afterglows lasting for days afterwards. It feels dirty at low doses....but if you combine a medium dose with some nitrous you will know true ecstasy

 

[3dempty]

I have heard dxm has been very helpful with tianeptine sodium