Comment · Mon, May 11, 2015
4-FA and tianeptine
Original post in this thread
baronjpetor · 0 points
I've found that tianeptine, taken before 4-FA, seems to cancel (or at least decrease a lot) 4-FA's effects.
Am I the only one or does anybody have a similar experience?
What they were answering
baronjpetor · 1 points
Sure, I had it clear that tianeptine is not a SSRE as it was previously believed. However I don't see the link between its effect on opioid receptors (it's only a very weak mu-opioid agonist by the way) and your conclusion about why it should decrease the effects of 4-FA?
I didn't read any convincing explanation in this thread so far... Calling out /u/borax and /u/misteryouaresodumb...
u/MisterYouAreSoDumb
Tianeptine's main actions are modulating the glutamate receptors in the CA3 region of the hippocampus. It's essentially a signal transduction modulator between the various types of glutamate receptors; normalizing the scaling of the amplitude ratio of NMDA receptor to AMPA/kainate receptor-mediated currents. So it prevents stress-induced neuroplastic remodeling, which arises from excess calcium transmission into neurons. It also increases BDNF, which could be due to the opioid affinities.
As to whether or not it will decrease 4-FA's effects, that is complex. Could the modulation of the glutamate receptors affect the dopamine and serotonin release from the 4-FA? It's possible. It's also possible it will enhance it. More likely is that it would protect the brain from excitotoxicity a bit, because of the normalization of the AMPA/kainate/NMDA currents. However, you also have to take into consideration the increased load on the liver, since it is hepatically metabolized. If dosages are kept reasonable, that should not be an issue, though.