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Bromidol

Wikipedia says ketobemidone "also has some NMDA-antagonist properties."
128px-Ketobemidon.svg.png
It's not unreasonable to suspect that a ligand like 1 will follow suit. Infact, i'd say that it appears likely. The fact that the m-phenol analog of 1 is a μ-antagonist is in alignment with dissociative SAR's and not phenylpiperidine SAR's. The 2-phenethyl products ofcourse are tremendously powerful opioids, and any NMDA activity in these will be cowering. Again, that only stands correct for the p-substituted products; the bare phenyl nucleus compounds lack analgesic potency.

Consider the following multiple choice question: Which statement best describes 1?

(a) μ-agonist.
(b) NMDA antagonist.
(c) None of the above.
(d) All of the above.

I'd say that (d) best describes 1 but this is purely conjectural.
 
haribo1 said:
^Even though it looks similar to things like meperidine, the potency of the p-methyl analogue is 1/2 the potency of morphine... Well, like F&B said, maybe something like a methoxy or ethoxy or something would be more potent.
Ring substitution of the cyclohexanone ring would also be interesting to investigate. After all, meperidine was the starting point for things like allyl prodine

SAR of meperidine analogues
Click to expand...

The methoxy analogs have been looked at in the paper I referenced already: p-cresyl > p-anisoyl > phenyl.

The ring methylation proposal just is alot easier to talk about than it would be to actually do it.
That probably accounts for 99% of the reason why it has never been done.
 
I got a suprise E-mail from Lednicer which I thought I would share. If you remember, If you remember, the simpler para-X-phenyl-cyclohexanone class, the strongest members were both the p-Br & p-methyl. Well, it seems that the super-potent bromidol was made 'as a stunt' (his words) since they knew that both the addition of a phenylethyl and a para-(X)-phenyl BOTH dramatically increased potency. He just put the two ideas together.
Well, the p-methyl analog of bromidol has never been made...

Now, he suggested that the importance in group-selection is simply atomic radius... so the AR of Bromine is 115... and the CH3 group? I don't know.... over to someone who does...
 
DarkMind said:
carfentanil its the most powerful opiate, it's used to sedate big animals like elephants
Click to expand...
Schmiedhammer in Insbruck (Austria) reported some morphine based compounds which have up to 1,000,000x the potency of morphine upon spinal or supraspinal administration, far exceeding carfentanil.
http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum

He also invented a compound that is 25x as potent as etorphine in the tail flick assay: http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum

Addidionally, fentanyl derivatives have been developed by BOC which are far more potent than carfentanil.

So your statement is clearly wrong; it might be right for the well known, scheduled opioids.

But these ultra-potent opioids are of little use except in specialized lab research where they have the facilities to handle such potent compounds. For recreactional purposes something like raceflaxeladol with a potency similar to morphine is much more practical and safe. And it's much harder to identify and economically manufacture an opioid equipotent to morphine than an ultra-potent opioid. Part of the reason is that most research has focused on maximizing potency, while hardly any work has been done on morphine-equivalent opioids.

We've seen in the past the bad consequences when ultra-potent opioids (3-methylfentanyl etc.) hit the gray/black market. We don't need a repeat of so many fatal ODs.
 
^ are you sure carfentanil does not express similar potency when administered via those or similar routes?
notably as well we do not really refer to those routes so if the compound you note is 1Mx as potent via such what is it via comparable routes
 
The German Bromidol patent by Lednicer is DE 2839891, and there's something strange: they disclose methods (Beispiel 6 following) to make pills and capsules and such containing Bromidol. These contain 30 - 60mg (!) Bomidol and were to be taken every 4 - 6h for pains like headache or moderate back pain. Neither the type of pain nor the dose does fit to the ultra-potent opioid Bromidol. What's going on here? Something's obviously wrong.
 
haribo1 said:
cyclohexanone.jpg


This much simpler molecule is supposed to be equipotent with morphine. Given that the synthesis is so simple, I can see this stuff turning up somewhere or other.
Click to expand...

Sorry to dig up this old thread but what is the name of that molecule. the pic is named cyclohexanone but thats not it and the link posted a few posts down is broken. could someone point me in the right direction please?
 
I don't think finding a chinese lab to syth one of these would be as hard as you might think. I ask a couple of them about making 10 kilos of N,hydroxymethamphetamine. Both quoted me a price (not exactly cheap but quite reasonable) without so much as a "WTF are you planning to do with that you fucking tweaker?". I had neither the cash nor the balls to follow through, ask sorta as a joke but they seemed to think this was just another order. But although I know for a fact both are legit that doesn't mean they might decide to turn scammer on something so obviously illegal (can't think of a more obvious analog). And I'm guessing if customs caught it you would get more than a love letter.

edit-hell, one of them e-mailed offering to match their competetors price, LOL
 
well for that matter you could also easily hire a hitman to kill somebody but that doesnt mean it is a good idea:\
 
amanitadine said:
well for that matter you could also easily hire a hitman to kill somebody but that doesnt mean it is a good idea:\
Click to expand...
True, but you would only need a gram of something so potent. It would fit in an ordinary letter so the chances of customs catching it are pretty slim. The chances you would get ripped off are pretty good, the chances of developing an opiate addiction from hell are even better.
 
There are a number of substituted 4-aminocyclohexanol's which have potency approaching Bromadol.

The synthesis is not that hard (not that easy either) but the starting compounds are easily obtainable....
 
fryingsquirrel said:
I don't think finding a chinese lab to syth one of these would be as hard as you might think. I ask a couple of them about making 10 kilos of N,hydroxymethamphetamine. Both quoted me a price (not exactly cheap but quite reasonable) without so much as a "WTF are you planning to do with that you fucking tweaker?". I had neither the cash nor the balls to follow through, ask sorta as a joke but they seemed to think this was just another order. But although I know for a fact both are legit that doesn't mean they might decide to turn scammer on something so obviously illegal (can't think of a more obvious analog). And I'm guessing if customs caught it you would get more than a love letter.

edit-hell, one of them e-mailed offering to match their competetors price, LOL
Click to expand...

I reckon chinese labs are going to be staying far away from opiates in comparison to stimulants.
 
hate to bump this thread up but it appears that this substance will become available from a vendor in the next month or two. Given that it is active at 1 ug, I feel like you could OD just handling this powder. I can just hear the bodies dropping now of the naive users taking keybumps of this stuff... Anyone else think releasing this chem is a bad idea?
 
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