4DQSAR
Bluelighter
- Joined
- Feb 3, 2025
- Messages
- 5,836
i think trying out Iboga might be a better idea than the mystery powder game
I think I see what you mean. I've read a few small studies and it seems that often there is at least one fatality. But these were generally people for whom the potential benefits made the risk worthwhile.
But however I slice up SR 17018, it makes no economic sense or scientific sense.
SR1017 has a Ki of 11 (morphine has a Ki of 14nM for comparison) so while it MAY benefit people consuming opioids of moderate potency, with potent ligands, there is a problem. Internization of receptors is the major driver of 'tolerance'.
You cannot 'rewire' that which no longer exists.
That's why I warned people that of the five chemists I've known who made fentanyl and broke 'rule 1', 2 are dead, 2 are (still) in jail and the last who was more of a hanger-on than a chemist was still in the acute phase of withdrawal after a year. For people in that position, substitution isn't a realistic option.
That's why my pragmatic response to the fentanyl/nitazene/4PP epidemic in North America that the 1c derivative of R-4066 should be explored. It's around x106 M in terms of analgesic activity with a half-life of 17.6 hours. Both figures from rodent models so these can only be rough estimates.
But to me it comes as no surprise that such potent compounds are essentially a 'one way street'. We don't consider what we mean when we say 'dependent' and 'tolerant' because in fact with all opioids two mechanisms compete but the second is only significant when high affinity/long mean receptor-occupancy time ligands are involved.
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