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Bromidol

Well, it IS unusual. The initial trials was with a a cyclohexanone ring 4 phenyl, 4 dimethylamino cyclohexanone. That was equipotent with morphine. Interesting how such a simple structure can be so powerful (then again, tapentalol has only got 1 ring in it, and thats quite potent).
 
I am a fool! Out by a factor of 10, shoot me!

On rereading the papers by the inventor, I see that bromidol is NOT 1200x morphine in potency, but 12000x! So, the raecemate is just over 6000x morphine. So, unlike ohmefentanyl, isomer seperation is not so important. I mean, 1g is going to be as strong as 3Kg of heroin!

He also mentions an Etorphine analog in which the butyl chain running from the 8 position is replaced with a 3 phenyl propyl group as 'a super potent oripavine'. I mean, Etorphine is 10000x morphine, so how bloody strong is THIS analog!!!!!
 
Oh, that bromine is important. Chlorine analogues are about 100x less potent. I expect that it's the bulk of the bromine thats more important than it's electronegativity. Can anyone think of something with a similar size? I mean, I don't think anything except halogens were tried, but what sbout pseudohalogens? Nitrile, trifluoromethyl, methoxy (I'm thinking of etonitazine here).
 
Looks like a super easy molecule both to synthesize and separate diastereomers. I question its potency though because if Haribo-! is correst this traslates into low picomolar to even femtomolar MU binding. I don't think the biologists can even measure femtomolar numbers in a binding assay, they have great trouble with picomolar, and even single digit nanomolar numbers come back slightly different every time because of the errors in measurement using the radiolabelled test ligand. We are at the borders of reality gentlemen.
 
I have no intent of making the stuff but the potency & unusual shape that appeals to me. That etorphine analogue sounds interesting. If x12000 is the standard by which he's measuring, just how strong can it be?
 
With the relatively easy synth and ultra potency, do you really think it's a good idea for this to get out there? With the R/C companies out there now with (what I assume are) well stocked labs and competent chemists, this certainly looks like something they could handle producing. A legal, ultra-potent opioid.

These opioids from distinct classes like these are all very interesting.
 
I'm just interested in the huge diversity of skeletons within the opioids. Now, we have an amine and a hydroxyl group & the cis isomer is the effective one. So, a simple way to do a partial crystalisation.
 
It's the trans isomer that is the most active, and the synth is not what I would call "easy" by any stretch.
 
Well if your looking for another group to replace the bromo group, I'd go with ethoxy as (etonitazene - a para ethoxy group para-substitute the most potent of the nitazene range and that group contains active drugs with all sorts of weird shit substituted
 
Ham-milton said:
With the relatively easy synth and ultra potency, do you really think it's a good idea for this to get out there? With the R/C companies out there now with (what I assume are) well stocked labs and competent chemists, this certainly looks like something they could handle producing. A legal, ultra-potent opioid.
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I think bringing out an ultra-potent opioid would be the stupides thing an RC company could do. Bringing out an opioid in the morphine potency class would be much more intelligent. But they are rare and hard to find. Besideas, what RC companies are left after WebTryp to bring out innovative stuff?
 
Even if a new class of opioids were to be found, how long do you think it would be before illegal? The gestapo works quickly. Also, i'm not certain on this but the class that the Bromidol structure is probably already covered in a patent somewhere. I just know that i've seen such analogs because cyclohexane-1-4-dione monethylene ketal has been used extenxively by researchers, deep down in the molecule mines. I know this because i have worked on simoilar structures.
 
Holy_cow said:
I think bringing out an ultra-potent opioid would be the stupides thing an RC company could do. Bringing out an opioid in the morphine potency class would be much more intelligent. But they are rare and hard to find. Besideas, what RC companies are left after WebTryp to bring out innovative stuff?
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There are certainly quite a few of them out there, though the majority are no longer US based.
 
fastandbulbous said:
Well if your looking for another group to replace the bromo group, I'd go with ethoxy as (etonitazene - a para ethoxy group para-substitute the most potent of the nitazene range and that group contains active drugs with all sorts of weird shit substituted
Click to expand...

Excellent suggestion, you obviously know what you're talking about.
 
Ham-milton said:
With the relatively easy synth and ultra potency, do you really think it's a good idea for this to get out there? With the R/C companies out there now with (what I assume are) well stocked labs and competent chemists, this certainly looks like something they could handle producing. A legal, ultra-potent opioid.

These opioids from distinct classes like these are all very interesting.
Click to expand...


When you're talking about synthesizing things that are extremely toxic, like sarin /VX nerve gas or the above extremely potent mu agonist, there has to be an airtight seal around all of the reaction vessels because it takes so little a dose of the compound that it can be inhaled as a vapour or an aerosol and cause acute toxicity. If your average Chinese lab went to make it in a custom synthesis, people would be ill or possibly worse because of not being equiped for such things. It would end up being a trail of death following wherever the chemical went. Once they start tracing who made the order you have an international incident...
 
fastandbulbous said:
Well if your looking for another group to replace the bromo group, I'd go with ethoxy as (etonitazene - a para ethoxy group para-substitute the most potent of the nitazene range and that group contains active drugs with all sorts of weird shit substituted
Click to expand...

I don't think so. With etonitazine, the ethoxy binds to another receptor site doesn't it? isopropoxy is 1/2 the potency, the methoxy 1/50th of the potency and so on. The thioethers are active, but much less so. The halogen isomers (clonitarzine, bronitazine) are only about x2 morphine in potency.

I'm thinking that the bromine (which is twice the potency of the chlorine) is more just a space-filling thingy.
 
fastandbulbous said:
When you're talking about synthesizing things that are extremely toxic, like sarin /VX nerve gas or the above extremely potent mu agonist, there has to be an airtight seal around all of the reaction vessels because it takes so little a dose of the compound that it can be inhaled as a vapour or an aerosol and cause acute toxicity. If your average Chinese lab went to make it in a custom synthesis, people would be ill or possibly worse because of not being equiped for such things. It would end up being a trail of death following wherever the chemical went. Once they start tracing who made the order you have an international incident...
Click to expand...

That wouldn't be good...I wonder if the Chinese government would ask for you to be extradited so you could be tried under Chinese law for killing their citizens...
 
^Very likely. Unless you had unbelievable amounts of money and connections, you would almost certainly be executed.
 
I doubt the US would turn one of it's citizens over to the Chinese to be executed over something like this. Anthrax letters, torture- even then it's not certain, but this? Probably not.

I mean, they must be able to handle it- remember "pharaohfentanyl"? LOL
 
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