Bromidol

[Bondmaker]

Undetailed

It's the trans isomer that is the most active, and the synth is not what I would call "easy" by any stretch.

Actually, the horrifying thing is, this molecule is ridiculously easy to synthesize. Here is a synthesis that would only be understood by chemists and is not a "threat" of giving anything to anybody.I think this should be sufficiently cryptic enough, not to go against our "no synthesis" rule

!) protected cyclohexanedione, 4-Br-phenyl Grignard (yes, it exists). Barbier type reaction with appropriate imine.
2) Deprotection
3 Obvious Grignard

I would hate to see anyone ever do it and put it one the street, just contemplating anything that toxic makes me queasy. The formulation would be bound to go wrong in the hands of amateurs, and result in many deaths.

 

[Smyth]

There's no point in discussing what I will call "fantasy synthesis" because a) the details are in the literature already, and b) there are more than one way most compounds can be made (implying that its hard to keep it "in-brief" since the discussions will go back-and-forth like a game of racket sport).

The formulation would be bound to go wrong in the hands of amateurs, and result in many deaths.

Precisely, why I said it is not that "easy" to make.

 

[haribo1]

I would sure like to know just what the working enviroment for the guys researching ohmefentanyl were. of course, the patents and papers don't list any special precautions...

 

[fastandbulbous]

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

Just watch the rabid, real foaming-at-the-mouth sort of frenzy of blood lust in US politicians when the holy 'War On Drugs' is incited. They burn with the sort of zeal that make Al-Quiada look like dilitantes by comparison.

Hell yes they'd ship one of their citizens down the Yangtse without a paddle if it was to help deal with the Growing Internet Drugs Menace (tm!). In the late 60s/early 70s, that great leader Richard Milhouse Nixon wanted the death penalty introduced for dealing acid (he might have said it during one of his depraven drunken binges, but say it he did). This is just a logical extension; if they can't off their own druggies, why not franchise it out to those who will (and not even expect a trade deal for doing so!)? These asre the final days of another desperate man in the White House, who lots want to see the back of - he even managed to make Tony Blair responsible for Iraq (MI5 say the've got WMDs, that's good enough for us, don't need to bother with the pics etc ), although to be honest, Tony Blair had already started to look like he was well on the way to a helter-skelter moment, this was his opportunity to be remembered (a wiser person might have just been happy with the Northern Ireland peace agreement, but nooooo...)

Anyway I digress (a bit too much). Yes they'd extradite you to China. Why fuck up a massive international trade over some druggie.

 

[haribo1]

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.

 

[Holy_cow]

^any references for this?

 

[fastandbulbous]

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.

Now that is so close to being an NMDA antagonist that I'd reckon any analgesic effect in rats rtc would be due to it's dissociative effect. That structure is effectively covered in a paper on PCP SAR studies I read qute a while ago (mentions alterations in potency by a) changing the amine group from a 1-piperidyl & 2) moving the keto group of ketamine around the alicyclic ring

 

[Smyth]

Now that is so close to being an NMDA antagonist that I'd reckon any analgesic effect in rats rtc would be due to it's dissociative effect. That structure is effectively covered in a paper on PCP SAR studies I read qute a while ago (mentions alterations in potency by a) changing the amine group from a 1-piperidyl & 2) moving the keto group of ketamine around the alicyclic ring

I disagree with the above comment.

It's the whole underground team on the scene, i'm letting off steam, go and ask Mr Bean, things aren't always how they seem, these insults look real mean, your comments have been seen, Requiem for a Dream....

 

[haribo1]

So, the p-Me or p-Br are the most potent, 50% as active as morphine. That's interesting given it's such a simple (and legal) compound.

 

[Canis aureus]

so, there it is... strikingly (shrinkingly) simple compound(s).

 

[DarkMind]

carfentanil its the most powerful opiate, it's used to sedate big animals like elephants

 

[skoat]

The thread is about a thousand times cooler than anything in other drugs.

Go College.

 

[MattPsy]

Smyth: I just read the full text of the paper you quoted - yup, it appears they are not the work the work of an NMDA antagonist disassociative, if naloxone reverses the effects of them - but F&B didn't say a NMDA antagonist - he said disassociative, which has a wider scope.

This could potentially include opioids that are selective for kappa, could it not? I don't think i'd want to take a long duration kappa agonist... like Salvia-XR. ugh.
I'm gonna start reading the references given. I'd give that reference a lot more weight if it had receptor binding figures.

 

[haribo1]

Oh, that etorphine analog that Lednicer compared his stuff with is called 7-pet. I cannot find a lot of information on it, other than it's not specifically outlawed anywhere.
Thebaine from codeine, now that would be a useful step...

 

[Canis aureus]

C8813

If something regarding C8813 tells about general receptor activities in this group, then there is practically no kappa agonism present ( in -cyclohexanones, -nols)...


http://www.ingentaconnect.com/content/els/00243205/2003/00000073/00000002/art00263

http://www.ihop-net.org/UniPub/iHOP/pm/9694361.html?pmid=12738037


MattPsy: Naloxone is μ-opioid receptor antagonist per se

 

[MattPsy]

Yes but it also has antagonist activity at kappa and sigma, which is why I said what I did. It was just a suggestion .

 

[Ham-milton]

Salvia XR? Isn't that the trade name for Cyclazocine?

 

[Smyth]

Smyth: I just read the full text of the paper you quoted - yup, it appears they are not the work the work of an NMDA antagonist disassociative, if naloxone reverses the effects of them - but F&B didn't say a NMDA antagonist - he said disassociative, which has a wider scope.

This could potentially include opioids that are selective for kappa, could it not? I don't think i'd want to take a long duration kappa agonist... like Salvia-XR. ugh.
I'm gonna start reading the references given. I'd give that reference a lot more weight if it had receptor binding figures.

Ok, I thought about this proposal for a brief time after you made the comments.
I didnt shove in an immediate response because i'd only just finished reading the abstract.

Further work on selected analogues shows these agents to be classical opioids.8 Effects of these compounds can, for example, be reversed by administration of naloxone. We consider this at least presumptive evidence that these interact with the same receptors as do classical narcotics. This obervation is at first sight surprising, since the compounds in question differ markedly from the connectivity posited by Beckett and Casey. Closer examination, however, shows topological similarity to the prototype narcotic meperidine. Comparison of Drieding models of 1 and meperidine, wherin the phenyl groups are axially disposed,9 allows direct superposition of carbonyl oxygens and nitrogen. It is of note that the aromatic rings will then occupy the same plane with about 0.5Å separation. While it is tempting to adduce physical significance to this observation, more detailed physical data is needed regarding the molecular pharmacology of these compounds. The topological significance does, however, serve to rationalize the activity of the above agents.

I would just strike the compromise that they are likely to be mu-agonists with co-joint NMDA antagonist activity.

 

[haribo1]

^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

 

[fastandbulbous]

Smyth: I just read the full text of the paper you quoted - yup, it appears they are not the work the work of an NMDA antagonist disassociative, if naloxone reverses the effects of them - but F&B didn't say a NMDA antagonist - he said disassociative, which has a wider scope.

This could potentially include opioids that are selective for kappa, could it not? I don't think i'd want to take a long duration kappa agonist... like Salvia-XR. ugh.
I'm gonna start reading the references given. I'd give that reference a lot more weight if it had receptor binding figures.

To be honest, it was NM|DA antagonist axctivity I was alluding to, but it appears I stand corrected