Opioid potency/molecular complexity, inversely proportional to euphoric potential.

[fastandbulbous]

^ I touched on that earlier. All things being equal though (which I assumed for the sake of arguement) then other factors apply.

Of course sopme drug groups have a different pharmacology profile altogether.

Yeah I'm not a big one on privelidged information. As regards pharmacology I don't want to fall into the 'better than you' sort of mindset, information is for everybody.

 

[sarbanes]

Maybe I'm in over my head here, but to me it sounds like this thread is failing to appreciate the complexity of opioid receptor subtypes and the fact that each of these compounds has a unique binding affinity profile across those subtypes...

For instance, say opioid agonist A has a 5 fold MOR affinity gain over opioid agonist B, which sounds super enough that you just might overlook a 7 fold KOR affinity. Since KOR agonism produces dysphoria, opioid A would likely produce LESS euphoria than opioid B, despite increased MOR affinity...

Of course that's an enormously oversimplified example that doesn't even tip the hat to gamma, delta or sigma opioid receptors, nor does it even cover a respectable fraction of MOR and KOR function.

I guess my point is, you can't boil "potency" down so simply, it's a very complex interplay, as others have mentioned it even extends into the realm of histamine and NMDA receptors.

Yup, and imagine taking the implications of that one step further. Imagine that by activating different subtype (clones), in differing degrees, results in not necessarily only an additive effect, but perhaps a radical change in the quality of the effect. Each quantize level of intensity and combination of subtype activation is potential to spell out a specific combination. Millions of possibilities here. Bring that one steep further, and imagine given combination effects people differently not only because of brain/expatiation, but of need and desire, and frequency of use, and just plain genetics. Its not quite as mind boggling as imagining how large the universe is, but still. There are so many possibilities, that the only thing that astonishes me, is when experts are totally surprised at new findings (which don’t necessarily fit into neat theories). Being good scientists, they should realize that because there is so much we don’t know, nothing can really be ruled out (unless you can in fact control for what you are ruling out). Even then, lets say there is a law higher in order than science (as we know it). Then we may never get the ultimate truths through scientific experimentation/replication alone.

 

[haribo1]

I'm wondering about taking ketobemidone & adding a 4 fluoro grouping next to the meta -OH. I think it would retain activity & if you read the MoDA carefully, you will see that it's legal...

 

[sarbanes]

I'm wondering about taking ketobemidone & adding a 4 fluoro grouping next to the meta -OH. I think it would retain activity & if you read the MoDA carefully, you will see that it's legal...

Administrative Law is largely arbitrary, so nothing is really safe. Its like, "I should this, therefore this is that."

 

[adder]

Of course that's an enormously oversimplified example that doesn't even tip the hat to gamma, delta or sigma opioid receptors, nor does it even cover a respectable fraction of MOR and KOR function.

And what are gamma receptors? Sigma receptors aren't considered opioid receptor subtype anymore, this has been proven by showing differences in structure.

Well, I snorted 30mg and was as high as a kite, I wouldn't be very high from 30mg of morphine.

How is your tolerance to morphine? And to what degree is there a cross-tolerance between ketobemidone and morphine?

 

[haribo1]

I had no opiate tolerence, or at least very little, but I tried 30mg of morphine one day & got very little (snorted) then ketobemidone the next day and was battered by it's effects. I would bet that esterifying that -OH would make the stuff pass the BBB much faster & allow the freebase to be smoked a la 'brown' number 3 heroin we get in the UK.

 

[fastandbulbous]

Administrative Law is largely arbitrary, so nothing is really safe. Its like, "I should this, therefore this is that."

The UK MoDA is based quite entirely on chemical definitions of what is a controlled drug, so legal wranglings over a compound are all within their chemical make-up. This means that any person fairly compitent in organic nomenclature can determine what does & doesn't fall within the MoDA.

Things like the US analog act are for the laywers as they're as clear in their definitions as a muddy puddle water

 

[sarbanes]

Is there any correlation between the freebase of said compound being a liphophyllic oil at room temp, and its rate/ability to cross BBB as a salt, in comparison to salts of random freebases which are solid (room temp), but still lyphophillic?

 

[fastandbulbous]

It's more to do with it's dissociation constant at physiological pH. The freebase can be as fat soluble as you want, but if it exists in soln almost exclusively in the ionic state. it's going nowhere. It's actually a combination of the two, but one predetermines the range of the other.

Luckily, most drugs are either acidic (-COOH, -SO3H) or alkaline (NH2) so form salts, but ones that are nowhere near totally ionic in solution

 

[In the Eyes of God]

carfentanil I hear produces relatively little euphoria

ROFLMAO as if theres a HUMAN ALIVE whose ever used Carfentanil, get real.

Im so sick of hearing this shit. "YA MAN I WAS BUMPIN CARFY FOR 6 MONTHS STRAIGHT YO"

I remember when Negrogesic from this board, supposedly a well respected guy, tried to tell me he used Carfentanil while in the hospital. Said he got a hold of a vial of it. ROFL hilarious, since Carfentanil isnt used in hospitals.

No ones used it, no one can tell you how euphoric it is. Anyone who tries to tell you, is a LIAR. People need to be less gullible on the internet. 99% of people on the internet lie once every 5 minutes.


Now on the otherhand, I have personally used >95% pure beta-hydroxy-4-methylfentanyl HCl salt and can tell you its as euphoric as heroin in my comparisons. Ive also used highly pure heroin HCl while in Colombia, im talking uncut south american #4

Theres some REAL feedback for you.

I think the euphoric potential of an opioid depends entirely on how rapid it crosses the BBB, and how mu-selective it is. The more mu-selective, the better.

I also beleive that delta-ANTAGONISTS reverse respiratory depression, therefore I beleive if you can get a hold of an opioid with a pharmacology of being a mixed mu-agonist and delta-antagonist you will have a potent analgesic with minimal respiratory depression. The ONLY compounds ive seen posessing these qualities are some peptide opioids, forget there names as that was ages ago I developed this hypothesis. Theyre legal though. Just contract an overseas peptide company to produce them for you, theyre very simple, I think they were made up of less than 10 amino acids, so theyd be easy to produce from scratch for any decent peptide synthesis custom manufacturer.

 

[In the Eyes of God]

Ummm personal experience Fentynal 75mg patches never did a thing either for euphoria nor pain nor make one sleep. and I would take/use up to 375mg a day..but then again I didnt bang it or eat it... hmmms. and then the morphine take doses of anywhere from 300 to 600mg a day and straight orally , 99% experience great euphoria and also does wonders for my pain.

you were UNDERDOSING FENTANYL BY FAR thats why it did NOTHING for you. 1.5 MILLIGRAMS of Fentanyl orally is equivalent to 80mg of Oxycodone orally. people have exaggerated the potency of Fentanyl by FAR. Anyone who takes 100mcg of fentanyl and says they got high is a fawkin liar. Straight up plain and simple. Fentanyls potency is exggerated massively.

Also your listing it as MG's, you were taking MICROGRAMS. MICROGRAMS is written as µg or mcg, not mg - thats MILLIGRAMS. No way you were taking 375mg a day, youd be dead 50 times over.

 

[haribo1]

Now on the otherhand, I have personally used >95% pure beta-hydroxy-4-methylfentanyl HCl salt and can tell you its as euphoric as heroin in my comparisons.

4 methyl? The one that's MUCH harder to make than the 3 methyl (and less potent), sir, either you were sold something else AS that compound or your being 'less than absolute with the actuality'.

 

[mad_scientist]

ROFLMAO as if theres a HUMAN ALIVE whose ever used Carfentanil, get real.

Im so sick of hearing this shit. "YA MAN I WAS BUMPIN CARFY FOR 6 MONTHS STRAIGHT YO"

I remember when Negrogesic from this board, supposedly a well respected guy, tried to tell me he used Carfentanil while in the hospital. Said he got a hold of a vial of it. ROFL hilarious, since Carfentanil isnt used in hospitals.

No ones used it, no one can tell you how euphoric it is. Anyone who tries to tell you, is a LIAR. People need to be less gullible on the internet. 99% of people on the internet lie once every 5 minutes.

Carfentanil is used in veterinary medicine for tranquilizing large animals. Brand name is Wildnil.

Etorphine is also used for the same purpose, brand name is Immobilon.

So both drugs are available to some people, maybe a bit more difficult to get than veterinary ketamine, but by no means impossible. Diluting it appropriately for safe use by a human might be a bit sketchy but could be done...

 

[haribo1]

Carfentanil HAS appeared on the black market, at least in Germany. It was not popular. Dihydroetorphine is used as a regular medication in China. It comes in 50ug pills and is often used by addicts who cannot access their normal supplies. If it's 1000x morphine, then 50ug equals 50mg of morphine, right? I know people fun around with the idea of 'blotter' opiates, but windowpanes might work well since, with the addition of more water, they would go right into solution...
As for carfentanil in hospitals, well, I don't know about EVERY country in the world. It's not used in the UK or the US which isn't to say it isn't used in other countries. I know of South Africans who have liberated Wildnil from the CDC and abused it. Simply place 1g into 1l of dH2O and voila, a solution thats as strong as morphine...

 

[fastandbulbous]

Vets in this country use Immobilon (etorphine), but it always comes with the reversal agent as it's so potent in humans (it's nowhere near as potent in most other species).

It's a CD, but vets are notorious for having piss poor security (I've seen a vets where the CDs were kept in a locked wooden cupboard - a one lever lock ffs)

 

[haribo1]

Etorphone = M99, Diprenorphine =M5050 (for the pedantic)