My opioid chemistry blog

[4DQSAR]

I'm actually surprised that nobody seemed to reaad the link to the patent on tianeptine analogues I posted.

Some are far more potent than their parent... and it's ONE STEP from a commercially available precursor.

ONE.

Also, I'm pretty sure of two things. One is that none of those analogues are legally controlled and the two precursors look totally innocent seeming.

On the other hand, for it's potency, it appears tianeptine dependence is viscious - but on the other, isn't tianpetine being sold as 'gas station heroin'? Certainly not something I would wish to be associated with, but if I can find that patent, so can others...

 

[4DQSAR]

3

Pharmacology Thread 'A new class of mu-opioid receptor agonists (tianeptine derivatives)'

Nov 10, 2024

US-2017217913-A1

https://patents.google.com/patent/US20170217913A1/en?oq=US-2017217913-A1

I'm not surprised that researchers have gone on to establish the QSAR of MOR agonists thar are based on tianeptine, It was @fastandbulbous who accurately described the chemistry of such compounds as having a certain element of 'black magic'. [1229] onwards lists the EC50 of some of the compounds covered by the patent. Example 83 appears to be the most active.

[1230] onwards lists activity relative to the prototype (tianeptine) and several 'rules' are divined to estimate said activity.

While...

• 3DQSAR
• Replies: 4
• Forum: Neuroscience and Pharmacology Discussion

 

[Rectify]

NUCI
N,N-diethyl-1-(1R)-phenyl-1-oxo-(2-(2R)-aminocyclohexyl)propane

 

[marcoman]

Oxy and clonazapam was my holy grail. Fkn doc stopped my clo' last year. I guess I have to be somehwar glad she didn't cut off my oxy. Shes still a bitch. I've been on the hunt (i'm in the USA) to get my k pins back but its almost impossible here. Fck, it's almost impossible to get any opiod OR a benzo here ins states now. Docs here choose their poshy careers and let peole suffer. I'm just waiting for her to cut off my oxys and suggest some shit drug like gabapentin or fkn Norco.