Loperamide -> 4 Day Smack
« on: January 10, 2010, 08:57:23 PM »
Thanks to beebo from the Hive & Wetdreams...
Loperamide is an opioid anti diarrheal, structurally similar to methadone, but not usually a compound that is psychoactive.
From wiki: "Loperamide is an opioid-receptor agonist and acts on the μ-opioid receptors in the myenteric plexus large intestines; by itself it does not affect the central nervous system like other opioids."
Well, let's change that, shall we?
First off, beebo discovered that mannitol has been used for some time to shrink the endothelial cells of the blood brain barrier to let things in to the brain which might seem like a bad idea... Exposing the brain to the unfiltered blood soup & all. Well, it's been done for decades now with cocaine as the typical cutting agent & they use this also for priming heart/lung machines during bypass so one might surmise that there's something else keeping the brain protected. As of this post, I'm unclear what that system is. Perhaps things still need a proper transport mechanism? If you have any information about that issue, please post.
Now that we've used mannitol about 2 hrs before hand to prime the BBB for passage, we need a proper transport mechanism for the loperamide.
Polysorbate 80 is that mechanism. Thank you again, beebo.
Mixing PS80 & loperamide under dry conditions causes nanoparticles to form. Basically, the PS80 encapsulates the loperamide. The brain sees the PS80 as usable fuel. These are taken up, enzymatically cleaved, exposing the loperamide & the lope binds to u-opioid receptors in the brain instead of the gut.
IV administration is choice for this however it's told to be inactive orally.
The potency is said to be near on par with morphine, the reported feel is much like demerol with an activity period often lasting 3 - 4 days.
The product can be easily acylated to yield a drug closer to heroin in potency with the same duration.
Now, it's up to you to learn how to extract your loperamide & find PS80 that isn't mixed with PEG & source your mannitol.
Enjoy.
Credit due to beebo (that insane fucking moose) for breaking the paradigm open & to jon for the detailed research into SAR studies, efficacy tweaking & acylation to stronger analogs.