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Designer opioids?

Yeah seriously. Even though it isn't a partial agonist like tramadol, it is still quite weak as a mu-agonist and has some other pharmacological activity outside of mu-agonism. Even if it doesn't have the serotonin reuptake properties on either individual isomer of o-des, one of the isomers has norepinephrine reuptake inhibiting properties giving more side-effects at higher doses like tramadol. So with a high opioid tolerance I'd figure it'd be like tramadol with there would be minimal opioid effect and larger non-opioid effect making it not that appealing for tolerant users.
 
All the discussion about ethics I think is strange... The only real "ethics" I think involving RC vendors or any drug dealers is simple. Be honest about the chemical and its purity, and give people what they paid for. As for selling very potent and powerful drugs, it's up to the user to not be a dumbass. If chemical name and exact purity are known, only the user can be held accountable in the case of an overdose. If, for example, you sell fentanyl analogues, this is totally ethical (legality aside). Sellers/dealers/vendors need to be 100% honest, and users need to be informed and aware


Turing Machine said:
As for acetylated hydromorph analogs. IV hydromorphone is awful. The high is almost nonexistent and all "rush". The withdrawal is a complete nightmare almost on the level of a precipitated withdrawal from taking a high dose of buprenorphine. I've experienced both and they were both far worse than methadone or heroin withdrawal. Oral hydromorphone isn't anywhere near as useless.
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First off, IV hydromorphone is awful? You're awful! J/k but seriously do you think orgasms are awful too? Secondly, you can acetylate it? Good god..... I've experienced the difference between morphine and diamorph, morphine being blah and diamorph being jizz-in-my-pants-godly, I can't even imagine what hydromorphone would turn into.... Probably the most intensely euphoric rush-y opioid ever that would make tar heroin look like darovcet
 
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Spooky Snacks said:
The best opiod on the face of the planet is heroin.

I do not see a more qualified alternative being created nor discovered in the near future.
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This is all subjective but in my opinion I would definitely say IV oxymorphone is MUCH more euphoric than heroin... lasts 8 solid hours at least also. A close second is IV hydromorphone, the duration is very short but the rush many people would say is better then pure pharmaceutical heroin.

Also, I personally haven't tried any of these new RC opioids due to a high daily dose of methadone, but from what I've heard most, like MT-45, are not very euphoric. There is one I have heard is actually very nice and surprisingly euphoric, acetyl fentanyl, but sadly when RCs like that hit the scene they are followed closely by reports like these... http://www.forbes.com/sites/davidkr...-on-deadly-new-designer-drug-acetyl-fentanyl/
 
RedRum OG said:
All the discussion about ethics I think is strange... The only real "ethics" I think involving RC vendors or any drug dealers is simple. Be honest about the chemical and its purity, and give people what they paid for.....
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This itself is one of the major arguments toward legalisation (or some drugs. I'm not going to example drugs which should or shouldn't be - it'll start a flame-war and for another thread). One of the biggest risks involved in (and for the end-user ultimately ingestion of) clandestine synthesized drugs are the fact that at no point along the development process any form of quality control is ensured! (except Bubba there possibly sampling the product - not exactly following standardised drug development protocol - R&D, pre-clin, clinical phase I > VI, blah blah, lol 8( ). Leading to a multitude, too many to list, of possible complications ...... Governmental control/production/oversight (take your pick of how much control would be exercised) would eliminate all of these (not to mention the ridiculous taxation revenue they would benefit :\ ).

As I said, this is just one argument toward legislation.


Pillls said:
This is all subjective but in my opinion I would definitely say IV oxymorphone is MUCH more euphoric than heroin... lasts 8 solid hours at least also. A close second is IV hydromorphone, the duration is very short but the rush many people would say is better then pure pharmaceutical heroin.....
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In fact an enormous amount of time, man-hours and funding (from all levels - Government to Universities) are currently going toward R&D - in not just synthetic opiates designed with improved drug profiles ...... properties such as greater [receptor/pathway] selectivity/targets, drugs which offer wide[r] therapeutic index [read: more forgiving], accommodating ROAs, of course reduced negative side-effects, etc. etc. :) - but "better" analgesics in general!

If anybody is looking for a career change, great strides are attempting to be made in analgesia - it's mechanism(s), biological and biochemical signaling/pathways, novel pharmacotherapies and the (seemingly increasing effect of the) psychological aspect associated. A fascinating field to be a part of, well, imo! ;) =D




Edit: Just re-read my post, I sound like a fan-boi trying to recruit. lol. It's basic, personal enthusiasm with the field, that's all :)

Pillls said:
....like MT-45, are not very euphoric. There is one I have heard is actually very nice and surprisingly euphoric, acetyl fentanyl....
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MT-45, this is a new one to me. A bit of research is in order tonight as it seems quite interesting - a piperazine derivative with opioid analgesic properties.
 
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Well you could end up with the shit storm that pretty much is responsible for the US analogue act, MPPP or more correctly the byproduct of piss poor synthesis MPTP. MPTP aka 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine. A neurological toxin and precursor to MPPP. The neurological toxin that destroys dopaminergic neurons in the substantia nigra of the brain creating permanent symptoms of Parkinson's disease. I guess this may be part of the reason that many RC developers are shying away from opiate analogues, that and most will probably result in a flux of OD's if even an opiate type drug of 1/2 the potency of Morphine was available to the general public and uncontrolled. Just my 5 cents.
 
lovepsychadelics said:
Well you could end up with the shit storm that pretty much is responsible for the US analogue act, MPPP or more correctly the byproduct of piss poor synthesis MPTP. MPTP aka 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine. A neurological toxin and precursor to MPPP. The neurological toxin that destroys dopaminergic neurons in the substantia nigra of the brain creating permanent symptoms of Parkinson's disease....
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Hmmm, like I said, I got the story. Read a few papers (peered).

lovepsychadelics said:
....I guess this may be part of the reason that many RC developers are shying away from opiate analogues, that and most will probably result in a flux of OD's if even an opiate type drug of 1/2 the potency of Morphine was available to the general public and uncontrolled. Just my 5 cents.
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I would hazard a guess for a long time it changed people' s minds about RCs!! It is quite a sad story though imo. He wasn't exactly a huge drug lord nearing billions from this all.
 
acetylating hydromorphone gives an opioid with a similar "rush" but with longer "legs". Am i correct?
 
Tryptamite said:
acetylating hydromorphone gives an opioid with a similar "rush" but with longer "legs". Am i correct?
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http://en.wikipedia.org/wiki/Acetylmorphone

According to this (well-cited) wiki page, potency would likely be increased, but would be slower-acting, though I imagine that would only apply to non-IV routes. So, basically, yeah, you're right. This would be quite a doozy; I haven't heard of it hitting "the scene" anywhere, but it doesn't seem like it would be that hard to make if you had enough pure hydromorphone. You would apparently need acetic anhydride, which I know is watched, or acetyl chloride, the watched-status of which I am unaware.
 
If I have hydromorphone as a precursor, what am I doing fucking with it? I'm already pretty solidly on the wrong side of the law, and I'm always going to have enough both in itself and as an impurity sufficiently significant to ensure that the product is still illegal. Acetylating agents are pretty suspect, the authorities know what's going on with them.
 
I'm really not qualified/knowledgable enough on the topic of psychopharmacological chem, I'm just killing time in my chem 1 class while they're teaching 9th grade level crap, but the second I opened this thread, my first thought was that when I've gotten far enough into my knowledge of chemistry and access to supplies, I would be beyond fascinated to diacetylize oxymorphone. This thread is a cock tease because I'm on a monthly Naltrexone shot for another year. I hope one day this becomes a reality. Will probably be something temporarily available through Chinese vendors, like methoxetamine, and banned 4 or so months later.
 
There are literally 10s of 1000s of opioids patented. The evil, pure $$$ guys will just sell the strongest, whatever the death toll.
 
How would one go about altering existing opiates to emphasize euphoria rather than analgesia?
 
tantric said:
How would one go about altering existing opiates to emphasize euphoria rather than analgesia?
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AFAIK both euphoria and analgesia come from mu opioid receptors. Some analgesia can result from delta activation, but why would you want to change the euphoria:analgesia ratio. Instead it would be more rational to just make structural modifications to the opioid to make it more potent, if euphoria is what is being sought for.
 
mu1 - analgesia
Mu2 - Euphoria & impairment of breathing reflex.

That's why fentanyl has such a narrow TI for euphoria.

Sufentanil is VERY mu1 selective with a TI of over 12000
 
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