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Novel Fentanyl Analogue

cosmotroniks

cosmotroniks

Greenlighter
Joined
May 11, 2010
Messages
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Boulder, CO
I'm posting this up to see what you guys think: I may have designed a new fentanyl relative that's potentially 21,334 times more effective than morphine.

The theoretical ED50 would be 0.0006259 mg/kg, based on the Calaulated Molecular Refractivity and cLogP values. Now there are of course many other variables/factors involved in calculating drug effectiveness/likeness, and I could be way off here.

I need to perform some docking analysis on this baby and see what I come up with.

The CMR values progressively increase as halogens are added at either the 4-position on the primary phenyl ring, or at the para-position on the other phenyl ring (adjacent to the propionamide skeleton). Two iodine molecules at both of these positions with a 3-methyl substituent on the piperidine ring seems to give an extremely potent potential analogue. Time shall tell whether this will really work or not...

Here's an image of the skeletal molecular structure:
4-iodo-B-hydroxy-p-iodo-ohmefentanyl.png
 
How come / why is it you never read such opioids referred to as 'super-agonists' when that is supposed to be the official name of any agonist that is more effective than the endogenous ligand? Is there some reason it is not a super agonist? Is binding frequency over receptor conformation efficacy play a part in the nomeclature or something?


Supeudol said:
^ Very very interesting.. Can you ship me a sample of this fentanyl analogue? ;)
Click to expand...

Looking for a sure fire chemical method of suicide or the like are you? :P
 
What would be interesting to know is it's half life. I don't know anything about the metabolism of fentanyl, so I can't tell what your creation will be like in that regard. But generally short lived opioids are useful as anaesthetics because the duration and strength of the anaesthesis can be finely controlled. And many fentanyl derivates are short lived.

Besides, are there any theories as to what causes an opioid to become "of recreational value"? Strong activity at the µ-receptor is somewhat involved, but some highly potent opioids still feel less "nice" than plain morphine.
 
The only people who should be obsessed about super-potent opioids are those trying to sell them.

Really, Heroin is potent enough. Fentanyl is already overkill. Why even bother with something more potent?
 
cosmotroniks said:
I need to perform some docking analysis on this baby and see what I come up with.
Click to expand...

I'd be eager to see those results, as there ain't any structures of the µ-receptor published (at least none with free access to the crystal structure data) and a docking task would include, therefore, creation of a sophisticated µ-receptor model beforehand.

But go ahead, it would be very interesting, as I said before.


- Murphy
 
The definition of super-agonist seems a bit slippery to me e.g. Icilin is referred to as a super-agonist but what is the endogenous (or "natural") ligand for the TRPM8 channel...a cool breeze...a sprig of mint? In that case there is a reference ligand which is menthol - anything that activates TRPM8 with a higher potency or efficacy than menthol is a super-agonist.

Jamshyd though I do agree heroin is "potent enough" diazepam, psilocin, 2C-B and methylphenidate are all "potent enough" as well - but that does not discount attempts to increase their potency and improve their subject effects in hopes of producing superior compounds and learning about the SAR of their respective classes.
 
Jamshyd said:
The only people who should be obsessed about super-potent opioids are those trying to sell them.

Really, Heroin is potent enough. Fentanyl is already overkill. Why even bother with something more potent?
Click to expand...

Isn't it obvious? To see how fucked up we can actually get! ;)
 
^ Sure, I understand where both of you are coming from, but how far do you go before you decide that a compound's dose is so miniscule you might as well not see it, yet you risk a sure death by simply breathing in a few invisible particles carried with wind drag? I certainly wouldn't care for being around such a drug...
 
I see the MANY obvious arguements against such potent opiates.

BUT I personally would love to have a drug that each 10 nano grams (as in a billionth of a gram) is as or more potent then a gram of heroin (seeing as a decent dose of heroin for one without tolerance is 100 mg thus 10 doses per gram). this would mean one would only have to break that one gram into the billion doses they would get out of it and even with a half life of a few hours that would be a LIFE TIME of opiate doses for one person and probally all of their friends. I mean SHIT, a billion doses!.

YES of course it would be EXTREMELY dangerous in MOST hands but those with enough self control, knowledge and care would be able to utilize such a substance for great benefit not only of the recreational variety BUT for medical and pain usage and probally even for the tranquilizing of large animals (like elephants ) such as is the use of carfentanyl.
BUT THERE ARE MANY ISSUES BESIDES JUST STRENGTH ESPECAILLY WHEN IT COMES TO RECREATION VALUE SUCH AS HALF LIFE, THE RUSH, ADDICTIVENESS, COME DOWN, SIDE EFFECTS (LONG TERM AND SHORT)..ALOT TO THINK ABOUT HERE BOTH FOR SAFETY AND PRACTICALITY

Of course having been a regular heroin user for 8 years i am
very biaist on such issues. I actually like fentanyl alot even with heroin but not really into the realitively weaker opiates ANED HONESTLY EVEN OXYCONTIN DOESN'T DO SHIT FOR ME T0 MAKE IT WORTH WHILE AND THE PRICE...I DONT KNOW HOW PEOPLE SPEND $20 ON AN OXY 80 LET ALNOE FUCKING 80 IN SOME PLACES WHEN A DIME BAG OF STREET H (.1-.15 GRAMS) WHICH HERE IN CHICAGO IS USUALLY 10-30 % PURITY HAS WAY MORE OF A KICK.

SORRY ABOUT RAMBLING AND PLEASE ASK FOR ANY CLEARIFICTIONS ON MY PIOUNTS CAUSE I AM SMACKED OUT OF MY MIND RIGHT NOW
 
^ Well for one, it really doesn't stop at self-control. I imagine you'd need a proper laboratory with nanogram-caliber scales (for measuring out EVERYTHING involved) and a vaccume chamber or other such installments.

And this is all just to measure it (or its precursors) out. It really isn't as easy as you imagine. In fact I'm inclined to call this and similar fent analogues Chemical Weapons, and indeed we've seen them used as such. I doubt this would do much in terms of euphoria...
 
Dude Man said:
I see the MANY obvious arguements against such potent opiates.

BUT I personally would love to have a drug that each 10 nano grams (as in a billionth of a gram) is as or more potent then a gram of heroin (seeing as a decent dose of heroin for one without tolerance is 100 mg thus 10 doses per gram). this would mean one would only have to break that one gram into the billion doses they would get out of it and even with a half life of a few hours that would be a LIFE TIME of opiate doses for one person and probally all of their friends. I mean SHIT, a billion doses!.

YES of course it would be EXTREMELY dangerous in MOST hands but those with enough self control, knowledge and care would be able to utilize such a substance for great benefit not only of the recreational variety BUT for medical and pain usage and probally even for the tranquilizing of large animals (like elephants ) such as is the use of carfentanyl.
BUT THERE ARE MANY ISSUES BESIDES JUST STRENGTH ESPECAILLY WHEN IT COMES TO RECREATION VALUE SUCH AS HALF LIFE, THE RUSH, ADDICTIVENESS, COME DOWN, SIDE EFFECTS (LONG TERM AND SHORT)..ALOT TO THINK ABOUT HERE BOTH FOR SAFETY AND PRACTICALITY

Of course having been a regular heroin user for 8 years i am
very biaist on such issues. I actually like fentanyl alot even with heroin but not really into the realitively weaker opiates ANED HONESTLY EVEN OXYCONTIN DOESN'T DO SHIT FOR ME T0 MAKE IT WORTH WHILE AND THE PRICE...I DONT KNOW HOW PEOPLE SPEND $20 ON AN OXY 80 LET ALNOE FUCKING 80 IN SOME PLACES WHEN A DIME BAG OF STREET H (.1-.15 GRAMS) WHICH HERE IN CHICAGO IS USUALLY 10-30 % PURITY HAS WAY MORE OF A KICK.

SORRY ABOUT RAMBLING AND PLEASE ASK FOR ANY CLEARIFICTIONS ON MY PIOUNTS CAUSE I AM SMACKED OUT OF MY MIND RIGHT NOW
Click to expand...

A bit tangential, but I read a study detailing how opioids that are active in (very) small dosages don't develop tolerance nearly as quickly as, say, morphine. I'll look for the study, but maybe someone can comment on whether they noticed fentanyl took longer to develop a tolerance for.



This would mean that slightly less than .5 micrograms would be roughly equal to 10mg of morphine. Or, 468 nanograms in particular. (10mg morphine/21334 = .000468 milligrams)
 
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i agree, its practically a chem weapon. you would need a hazmat suit on when your cooking the stuff.

ok heres a senario. you make it, clean your lab, clean everything, spray everything with acetone and some chemical that distroys your analog here. scrub it.

miss some thats floating in the air duct or some shit and the next person that walks into your lab is a dead man.

now however much time and thought and obsession you put into your little project here was for fuck all because now your buddy is dead here on the floor.

congradulations. now go live with that.
 
I've had contact with a drug that's seen as fairly potent, but has a much more forgiving nature in that the toxic dose isn't also invisible (LSD) and know from experience just how easy it is to absorb a tiny amount without knowing it. For me it was the aerosol produced by drops of the soln getting onto a paper cut on my hand. Reckon I must have absorbed 100-150ug of LSD and was a giggling fool for the rest of the day. Now if that happens with the opioid; no giggling, no recalling an unusual event, just blue skin and a toe tag in the local hospital's morgue...

For fuck's sake, most people can't handle RCs with dosages under 10mg as they make an error; even using professional lab staff doesn't guarentee that no-one will get an accidental OD
 
YEAH..
a lot of very good points

in theory this potent of a drug would be great..... if ALL percautions were taken and everything worked out and doses were premade but the place of handling (during which full hardcore hazmat style suits would HAVE to be worn the entire fucking time) and cutting would be a very dangerous place for a VERY long time.

The ONLY good tyhiing about such a potent substance that would havbe a million or more doses per gram would be that (like i stated before) one could have a life time of opiates on hand oce it is succesfully seperatd into very low dose capsules or pills with proper binders and such or easily measurable highly diluted liquid.

Though something that powerfull would consume your liufe and you would probally keep seeking a deeper high until in the stupor it would create most would keep upping the dose until it became fatal which already happens with heroin and fentanyl already and considering how much more potent this hypothytical drug would be such OD would be almost inevitable.

NOT THAT ANY OF THIS MATTERS CAUSE UNLESS ANY OF US KNOW A CHEMIST WITH A SCHEDULE ONE LICENSE WHO IS WILLING TO RISK SUCH A HARD TO ACHIEVE STATUS (especailly with all the beruactricy involved in obtaining one and the monitering once having one) AND RISK THAT STATUS FOR OUR SAKE OF GETTING HIGH OR MUTUAL FINANCIAL GAIN NONE OF US WILL EVER HAVE ACCESS TO SUCH AN EPIC SUBSTANCE. Probally for the better since some of the things i have heard that happened in the short time pharofentanyl was available as an RC... Honestly we were much better off back when the RC market was booming wiuth mainly tryptamines and phenethyl amines like from 2001-2004 right before operation tryp (those where good times with me and my friends consuming many many grams of AMT, 5meodipt (foxy), 2ct7, DXM, and many other fun things) cause for opiates heroin is probally the best anyways cause it has a great level of euphoria with a decent duration (though I often think it could be l0onger which is why i occcasionally like to add a little fentanyl to the mix but would rather do it my self than have an unkjown amount added by a "sneaky" dealer that thinkls they are slick and want us to think their dope is just that fire. Kind of like meth bomb pills, yeah I like meth or other uppers wiht MDMA sometimes by I would rather add it my self at what levels i want.
 
Your diagram is 8 different molecules

This is the win:

2ludima.png


(by virtue of analogy to the stereoisomers of fluorohmfentanyl, 4 of which inactive; read the paper)
 
Dude Man said:
BUT I personally would love to have a drug that each 10 nano grams (as in a billionth of a gram) is as or more potent then a gram of heroin (seeing as a decent dose of heroin for one without tolerance is 100 mg thus 10 doses per gram). this would mean one would only have to break that one gram into the billion doses they would get out of it and even with a half life of a few hours that would be a LIFE TIME of opiate doses for one person and probally all of their friends. I mean SHIT, a billion doses!.
Click to expand...

100mg of pure diamorphine HCl for a non-tolerant user??

Ehh.... I'll have to disagree with you..
 
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