Comment · Fri, December 19, 2014 · Ceretropic
Speculation: tianeptine + SSRI??
Original post in this thread
Bomb_Jack · 1 points
Hi all.
I was just wondering if it could be possible to take an ssri with tianeptine in order to cancel its serotonin uptake enhancing effect and so exploit its other benefits on the other single receptors (a bit like it's done with buprenorphine + samidorphan), or you would cause just an hazardous mess??
What they were answering
Bomb_Jack · 1 points
Oh really?
Didn't know it was mild.
Could you give me some more elucidations on the eventual MoA would take place, and what about the study I cited about SSRI and tianeptine canceling each other? (Maybe I'll post the link tonight)
u/MisterYouAreSoDumb · Ceretropic
tianeptine resulted in a normalized scaling of the amplitude ratio of NMDA receptor to AMPA/kainate receptor-mediated currents and prevented the stress-induced attenuation of NMDA-EPSCs deactivation. Both paired-pulse-facilitation and frequency-dependent plasticity remained unchanged. Both in control and stressed animals, however, tianeptine treatment strengthened the slope of the input-output relation of EPSCs.
So tianeptine modulates the currents between the AMPA and NMDA receptors, and prevents stress-induced attenuation of NMDA deactivation. Stress can over-activate the NMDA receptors, by preventing them from closing before too much calcium passes. This is called excitotoxicity, and is bad for your neurons. Tianeptine normalizes the currents between the AMPA and NMDA receptors, and prevents stress from leaving the NMDA channels open too long. That is how it decreases stress, and is neuroprotective.
It is not a DRI like some people are postulating.
So it modulates various glutamate receptors, which leads to increased dopamine in the nucleus acumbens. It also has mild opioid affinities, that usually only manifest at higher than therapeutic dosages. Go through that folder I posted. There are a lot of good studies in there.