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Opioids Brorphine

Feretile

Feretile

Bluelighter
Joined
Feb 2, 2022
Messages
361
I note a new class of opioid. It contains 4 of the 5 key moieties of a strong opioid, an ideal biosteric minimum and a clear metabolic pathway. If you go back to the 60s, Janssen produced some closely related compounds. In that case, a figure of x450 pethidine (x45 M) was given but that p-Br is important in obtaining the correct biosteric minimum so it may be more potent.

What I DID notice was that it is closely related to bezitramide (Bugodin™). While the n-propenoyl of bezitramide is suppose to be hydrolyzed by the GI tract, bezitramide is often given via bolus and so bezitramide rather than N-despropenoyl bezitramide will be the active drug.

Just to be clear, the x450 pethidine figure was based on writhing tests. The study was such a long time ago that the Straub tail-test wasn't used so it's hard to guess it's potency in man. It's of academic interest because it shows that rigid bioisosteres of the amide moiety produce activity and MAY go some way in understanding the active conformation of fentanyl.

Bezitramide it also interesting as an example in which a nitrile replaces the more common ketone moiety. Primary amides are also seen in related compounds and so their is a question over what these moieties DO. It may well be that they are simply space-filling. The methyl side-chain of methadone famously rotates one of the benzene rings and is a requirement, but it's not clear unless one overlays methadone & normethadone in a minimum-energy conformation. Dextromoramide shows a refinement of the specific rotation.
 
Brorphine is something I have not tried, but a good friend and Bluelighter accidentally overdosed on it several times. He said it has very little euphoria but is extremely strong, and told me not to touch it with a ten foot pole.
 
Worth knowing.

I am of the opinion that a legal dextromoramide (Palfium) analogue would be very popular. It's only x3 M in potency but that means it's easy to eyeball and since it's orally active (and produces a rush when used orally), it's safer overall. Of course, Janssen ONLY identified 1 compound of the class with significant activity.
 
It would be great if the gray/black market RC scene came up with something that is fairly safe. I mean there is O-desmethyltramadol, kinda surprised that hasn't totally disappeared. Seems like so many of the RC opioids are sketchy.
 
I'm truly amazed that whoever produced O-desmethyltramadol didn't read the papers and know that substituting the -OH with a -F solves all of the problems. No problematic SERT or NET activity AND it's x5 more potent than O-desmethyltramadol!

I am only too aware that fluorinating agents aren't too friendly but DAST and such are reasonable to handle. I mean I always try to devise routes using non-toxic reagents but DAST is about as safe as it gets in the -OH ---> -F step.

I presume that swapping the cyclopropylamine moiety with a pyrrolidine ring will work.

Of course, even the precursors to dextromoramide are controled.

I do have a design for something about x25M that is 1 step from commercially available precursors. The 1 step is also a name-reaction, so it's not like I have to GUESS that it will work.

AFAIK it's a class that hasn't been covered so I suppose people could keep altering it..... but even x25 is maybe too much. Eyeballing would not be ideal and I do not like solutions.... IVing is risky and leads to risky patterns of behaviour. Once 'the needle barrier' is broken, people often seem to shoot ALL of their drugs. Look at Russia. People IV MDMA.... so I for one do not believe their official HIV figures.
 
That's the thing, people are gonna be reckless, you can't stop that. If people could not be ignorant/reckless, an x25 opioid could be just fine, but people are gonna rack up lines, or shoot a bunch of it, because they're used to street drugs that are cut so you can do a big pile.
 
on it right now. no real euphoria and kinda boring. i feel itchy and no real sedation. will redose one more time and thats it. can anybody make a comparison between brorphine and fentanyl? can you distinguish them in a blind test?
 
I think I read bad stuff about brorphine, that it would induce irreversible tolerance by some kind of neurotoxicity at the receptor level. Unsure about whether this was correct - anybody having read/heard the same?
 
plumbus-nine said:
think I read bad stuff about brorphine, that it would induce irreversible tolerance by some kind of neurotoxicity at the receptor level. Unsure about whether this was correct - anybody having read/heard the same?
Click to expand...

I think you’re misinformed. After 2 days of trial I would say it’s a rather bad but not completely useless opioid. Think tramadol but a little less maybe.
 
Solid but boring, I think that is what you can get out of the fentanyl class.
 
I used brorphine for roughly 8 months or so. My friend almost died by quitting cold turkey and it was a very strange experience coming off of it myself. It wasnt bad overall.
 
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