Comment · Sat, January 3, 2015 · Ceretropic
how would you classify tianeptine as?
Original post in this thread
nutrop · 2 points
Since it is uncontrolled in the U.S., it is being sold as a nootropic, but it sometimes fall under as TCA (tricyclic antidepressant) and as analgesic affecting the opioid receptor.
What they were answering
DrMichaelPLudwig · 12 points
Legally it is an unapproved drug. Structurally it is a tricyclic. When doses at 12.5mg it exhibits little to no analgesia, but when dosed at say 50-100mg it most certainly is an analgesic. Tianeptine is far from a weak opioid; the recently observed binging affinities are misleading. Try taking 12.5mg of morphine and see if you feel any noticeable analgesia. Tianeptine has very favorable kinetics that allow it to rapidly absorb from the gut and quickly pass through the BBB. If you look at the structure of tianeptine, it shares some SAR with w-15 and w-18 which are both very potent opioids. If I were to guess, I would say that, in vivo, tianeptine undergoes rapid decarboxlation leaving the heptane tail that allows the drug to rappidly enter the brain much in the same way that the two acetyl groups allow heroin to enter the brain so fast. Cleaving of the tail leaves a pentane chain in its place. This could be the active moiety which may have a more favorable Ki than the parent drug.
u/MisterYouAreSoDumb · Ceretropic
Try taking 12.5mg of morphine and see if you feel any noticeable analgesia.
Uhh, it would certainly be analgesic... Oral Hydrocodone and oral Morphine are considered equipotent in instant release formulas. If you take 12.5 IR oral Morphine, you will feel it. It will be very strong for an opiate-naive person. It's certainly a lot more analgesic than 12.5mg Tianeptine.
I feel like I am taking crazy pills with all this Tianeptine talk. If the binding affinities are misleading, why does Tianeptine feel nothing compared to a real opioid? I've taken many different opioids, and Tianeptine has nothing on them. I know you have a friend that says IVing it is just like heroin, but that is not exactly convincing me; especially when we have the binding affinities, and I have taken various dosages of a bunch of opioids. They don't compare at all. So why should I consider the observed binding affinities misleading, when my own personal reactions, and the reactions of many people I know, confirm them?
the heptane tail that allows the drug to rappidly enter the brain much in the same way that the two acetyl groups allow heroin to enter the brain so fast.
Do you have any reading on this? The acetyl group transport is very well known, and there are a lot of studies about it. I am having a hard time finding references for heptane groups enhancing BBB transport similar to acetyl groups. The only thing I can find is that 2-aminobicyclo2,2,1-heptane-2-carboxylic acid (BCH) inhibits the BBB transporter for amino acids.