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Most pleasurable opioid based on pharmacology?

Morphine hands down with an antihistamine drug and clonazepam.
And asteroid could be about to colission with earth and I couldn't care less cause I'd be wrapped In that lovely warm fuzzy feeling.
 
DeathIndustrial88 said:
Tramadol is synthetic but it has some MDMA/Stimulant-like properties. It weakly releases serotonin.
It's metabolite is also a full agonist.

I haven't heard of too many other opioids that have the same qualities as tramadol.

Not exactly MDMA properties, but closest I could think of.

I loved tramadol in my early 20's before I discovered heroin. Most people hate it though and I can understand why.
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U mean ssri properties, isn't the same as a serotonin/dopamine releaser
 
nznity said:
Morphine hands down with an antihistamine drug and clonazepam.
And asteroid could be about to colission with earth and I couldn't care less cause I'd be wrapped In that lovely warm fuzzy feeling.
Click to expand...
Its good yeah.and good H,opium....long time ago we have wonderful vials-pantopon.Its a clear liquid for iv or im,which is max.pure phytoproducts.Contains all the alcaloids.50percent morphei.....fantastic stuff.
 
Nas47 said:
Its good yeah.and good H,opium....long time ago we have wonderful vials-pantopon.Its a clear liquid for iv or im,which is max.pure phytoproducts.Contains all the alcaloids.50percent morphei.....fantastic stuff.
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That's awesome. I remember reading about Pantopon in William Burroughs's books and thinking it sounded pretty special.
 
plumbus-nine said:
For me bromadol was fucking awesome. It's too potent to have it around all the times I see and probably hard to manufacture but they really should bring back bromadol solution. My plain guess is that it wasn't a pure mu agonist but maybe delta or some whatever exotic target which made it awesome but it was.
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Bingo - some people don't like BDPC or, rather, like the first 4 hours but not the next 8. I believe that this is because with that -Br present, the main metabolic pathway is N-demethylation and the desmethyl compound is a delta ligand. That is why I could never understand why vendors took so long to swap the -Br for a -CH3. The latter is slightly more potent (lower MW) and that 'magic methyl' provides a site for the body to hydroxylate & oxidise.... so it's just rocking pure mu activity.

For the record, it seems like the MOST euphoric opioids aren't generally the very potent ones. Tilidine get's VERY good reviews on Land der Träume. It has DRI & NMDA activity as well as being an opioid. Levorphanol & dipipanone both get amazing reviews - both have mu/DRI activity. Dextromoramide was amazing but kind of dodgy. Take 5 pills one day and get a good nod, take 4 pills the next day and pull a blue. Dangerous. I liked AH-7921 a lot (but only tried it once). O-desmethyl tramadol is OK if you don't have much tolerance.

I haven't tried brophene yet. It looks like the first novel opioid with a design from China,

There are still many more scaffolds that appear in patents but have not turned up as RCs yet.
 
I depends on the person/personal taste, I guess.

I'd say hydromorphone but morphine and diamorphine (real diamorphine, not heroin) are up there, too.
 
nznity said:
U mean ssri properties, isn't the same as a serotonin/dopamine releaser
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SSRI's don't have the ability to release serotonin as tramadol does.

Tramadol not only inhibits serotonin, but can release it as well (i.e. - MDMA, meth, etc..)
Of course this isn't going to feel exactly like the aforementioned drugs.
But tramadol is the only opioid I know of that causes serotonin release.
And most likely causes dopamine release, like all opiate/opioids do.

And technically, it'd be an SNRI/releaser and not just simply an SSRI.

"Tramadol is known to inhibit
serotonin reuptake and may induce serotonin release
at high doses (23)."

I personally found tramadol to be very stimulating & empathogenic (similar to MDMA in a way, but much more mild). Of course other opioids can feel this way at times too.
Some articles and scientists postulate that ALL opioids cause serotonin release. As well as dopamine release. But that's for another day.
 
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Actually, joint MOP/NOP ligands may be the most euphoric. Back in the 1960s a group of German chemists expanded the QSAR of etonitazene. By adding a chiral carboxamide (-C(O)NH2) to the methylene spacer, the compound was x4 more potent. Now I don't think it vastly increased MOP affinity, but I note that when overlayed with MCOPPB, the N: of the carboxamide overlaid the N: of the piperidine's nitrogen.

I think joint MOP/NOP ligands are more potent analgesics, may well be more euphoric & less dependence-forming. It SEEMS too good to be true....
 
DeathIndustrial88 said:
SSRI's don't have the ability to release serotonin as tramadol does.

Tramadol not only inhibits serotonin, but can release it as well (i.e. - MDMA, meth, etc..)
Of course this isn't going to feel exactly like the aforementioned drugs.
But tramadol is the only opioid I know of that causes serotonin release.
And most likely causes dopamine release, like all opiate/opioids do.

And technically, it'd be an SNRI/releaser and not just simply an SSRI.

"Tramadol is known to inhibit
serotonin reuptake and may induce serotonin release
at high doses (23)."

I personally found tramadol to be very stimulating & empathogenic (similar to MDMA in a way, but much more mild). Of course other opioids can feel this way at times too.
Some articles and scientists postulate that ALL opioids cause serotonin release. As well as dopamine release. But that's for another day.
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Idunno man, I'm high on morphine +pentin+6mg clonaz throughout the day
Feretile said:
Bingo - some people don't like BDPC or, rather, like the first 4 hours but not the next 8. I believe that this is because with that -Br present, the main metabolic pathway is N-demethylation and the desmethyl compound is a delta ligand. That is why I could never understand why vendors took so long to swap the -Br for a -CH3. The latter is slightly more potent (lower MW) and that 'magic methyl' provides a site for the body to hydroxylate & oxidise.... so it's just rocking pure mu activity.

For the record, it seems like the MOST euphoric opioids aren't generally the very potent ones. Tilidine get's VERY good reviews on Land der Träume. It has DRI & NMDA activity as well as being an opioid. Levorphanol & dipipanone both get amazing reviews - both have mu/DRI activity. Dextromoramide was amazing but kind of dodgy. Take 5 pills one day and get a good nod, take 4 pills the next day and pull a blue. Dangerous. I liked AH-7921 a lot (but only tried it once). O-desmethyl tramadol is OK if you don't have much tolerance.

I haven't tried brophene yet. It looks like the first novel opioid with a design from China,

There are still many more scaffolds that appear in patents but have not turned up as RCs yet.
Click to expand...
Sounds dirty, nothing like full mu agonism.
I still don't get why some ppl like tram more than morphine sometimes, it just plain sux man. I like nod off and dream while awake but tram, tapentadol and those opioids with snri properties don't give me euphoria. 🤮🤮🤮
 
Some people seem to really agree with tramadol, you either love it or it's nothing special. I am sure it comes down to individual metabolic factors in how efficiently you metabolize it into o-desmethytramadol (which is a much stronger mu agonist). Personally I don't get much from it, I can take 500mg and have no sign of lowered seizure threshold, and not much in the way of an opiate high, either. Whereas my friend, even in the midst of heroin addiction, would take 100mg and be nodding. he absolutely loved it. He took 150mg one time and said he was shaking so hard he thought he was going to die.
 
Glutethimide (and to a lesser extent pyrithyldione are CYP2D6 enhancers so they will increase the O-demethylation of codeine, oxycodone, tramadol and other prodrugs. p-aminoglutethimide is ALSO a CYP2D6 enhancer but it's a chemotherapy drug so I wouldn't touch it. What they do together is to reveal the QSAR of the CYP2D6 enhancing action.

Oh - and O-desmethyltramadol was a popular RC. It was banned after some scummy vendor cut it into kratom and killed some kids.
 
Feretile said:
Glutethimide (and to a lesser extent pyrithyldione are CYP2D6 enhancers so they will increase the O-demethylation of codeine, oxycodone, tramadol and other prodrugs. p-aminoglutethimide is ALSO a CYP2D6 enhancer but it's a chemotherapy drug so I wouldn't touch it. What they do together is to reveal the QSAR of the CYP2D6 enhancing action.

Oh - and O-desmethyltramadol was a popular RC. It was banned after some scummy vendor cut it into kratom and killed some kids.
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Gluthed was a hihgly popular like enhancer for codeine(probably same with tram) years ago.But i nave not any experience with this hypnotic.Then came rare and somehow sank.Even not sure is present now
 
For what it's worth, tramadol was wonderful for me (in the 300-600mg range) for many years through out my 20's. Practically a decade.
I preferred 400mg of tramadol over 10-20mg of hydrocodone any day.

But after getting into heroin & buprenorphine, it's like my liver metabolism changed and tramadol lost a lot of it's magic, even when tried again with no tolerance.

Haven't had it in a long while now but I'm assuming after getting use to more potent opioids, that my body chemistry changed and it stopped agreeing with tramadol (considering it wasn't just a tolerance issue).

A tram high started for me by being stimulating for about 2hrs and around hour 3 it became noddy, same exact nods that I'd get on heroin basically. Then another 4-6hrs of intermediate nodding/stimulation. I loved it.
 
Nas47 said:
Gluthed was a hihgly popular like enhancer for codeine(probably same with tram) years ago.But i nave not any experience with this hypnotic.Then came rare and somehow sank.Even not sure is present now
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I remember watching a documentary about heroin addicts in Sofia, filmed over a couple of years in the late 90s or early 00s (IIRC), which had footage of them using glutethimide/codeine on a pretty heavy basis. They actually seemed to get way more "fucked up" (for lack of a better word) from that combo than from IV heroin.

Parkisal(sp) was another drug they were shown taking in the documentary. I think that's biperiden... it seemed like more of a euphoric psychedelic than a hallucinatory deliriant in its effects, at least as they were shown in the film. I recall seeing a couple walk down the street, a few apart from one another, with a voiceover from the guy about how they communicated telepathically on it.
 
Nas47 said:
Gluthed was a hihgly popular like enhancer for codeine(probably same with tram) years ago.But i nave not any experience with this hypnotic.Then came rare and somehow sank.Even not sure is present now
Click to expand...

I'm just looking at the original 1954 patent. I've also looked at the synthesis of p-aminoglutethimide and it's totally different. Of course, I am VERY careful not to break any laws so I suggest that p-F glutethimide will be a CYP2D6 enhancer that is legal. In fact, if it loses it's sedative/hypnotic action then that is to the good since it will not fall under the PSA.

I've also closely looked at the PSA and do you know what - the inactive carbamate ester derivatives of controlled compounds are NOT covered. Why is this worth knowing? Because you can just hydrolize an active drug by boiling it in water. It's another league of complexity and it would need consideration for every single compound BUT it is possible.
JTemperance said:
I remember watching a documentary about heroin addicts in Sofia, filmed over a couple of years in the late 90s or early 00s (IIRC), which had footage of them using glutethimide/codeine on a pretty heavy basis. They actually seemed to get way more "fucked up" (for lack of a better word) from that combo than from IV heroin.

Parkisal(sp) was another drug they were shown taking in the documentary. I think that's biperiden... it seemed like more of a euphoric psychedelic than a hallucinatory deliriant in its effects, at least as they were shown in the film. I recall seeing a couple walk down the street, a few apart from one another, with a voiceover from the guy about how they communicated telepathically on it.
Click to expand...

Biperidin is an acetylchloline esterase inhibitor. I've heard of Polish people taking Artane (a related drug) & brandy to get the same result. It seems awfully risky.

Glutethiide/codeine is supposed to be an amazing high. I don't suppose you know if they got it as a prescription drug or if their are 'cooks' making it. It's a 1-pot reaction using very simple precursors BUT it takes 500-1000mg to work so one would not imagine it being profitable. That said, methaqualone is still HUGE in South Africa.

Those old school downers sound awesome but also dangerous. Ludes (Methaqualone), jelly bellys (Placidyl), meprobramate (Placidyl). I guess IF people would be prepared to pay £10 for each lude THEN it's profitable.....



FYI I loathe Hamilton Morris. He really does NOT understand the chemistry - he's JUST good enough to fool the average hipster.

Their IS a modern lude mimic called pynazolam. The problem was that synthesis was too complex (expensive).

ibb.co

pynazolam hosted at ImgBB

Image pynazolam hosted in ImgBB
ibb.co ibb.co

Flunitrazolam, nitrazolam, clonazepam & flunitrazepam do not have the same effect. In essence, it's a serotonin releaser and a gaba a2/a3 PAM - so it's action is unique.... BUT maybe nimetazepam IS similar. I know it's highly sought after & is usually consumed in clubs so it MAY be similar.
 
Feretile said:
Biperidin is an acetylchloline esterase inhibitor. I've heard of Polish people taking Artane (a related drug) & brandy to get the same result. It seems awfully risky.

Glutethiide/codeine is supposed to be an amazing high. I don't suppose you know if they got it as a prescription drug or if their are 'cooks' making it. It's a 1-pot reaction using very simple precursors BUT it takes 500-1000mg to work so one would not imagine it being profitable. That said, methaqualone is still HUGE in South Africa.

Those old school downers sound awesome but also dangerous. Ludes (Methaqualone), jelly bellys (Placidyl), meprobramate (Placidyl). I guess IF people would be prepared to pay £10 for each lude THEN it's profitable.....
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I think they got them from crooked pharmacists at that time, but I've read (probably in a UNODC report) of small-scale glutethimide "labs" that were busted in Hungary and Romania around 2005-06 – which is, not coincidentally, when they took off the market the last remaining formulations, like Tardyl (glutethimide/amobarbital/hydroxyzine 125/125/25mg).

Personally, I'd be thrilled to line up at dawn for the chance to pay 10 GBP per 'lude, at least a couple of times. I do have a suspicion that methaqualone has been exaggerated, but if it was replaced with Doriden or Placidyl, I'd be just as happy. You're right about the dangers, though; lots of teenagers died on Tuinals and Sopors in the 60s/70s.
 
JTemperance said:
I remember watching a documentary about heroin addicts in Sofia, filmed over a couple of years in the late 90s or early 00s (IIRC), which had footage of them using glutethimide/codeine on a pretty heavy basis. They actually seemed to get way more "fucked up" (for lack of a better word) from that combo than from IV heroin.

Parkisal(sp) was another drug they were shown taking in the documentary. I think that's biperiden... it seemed like more of a euphoric psychedelic than a hallucinatory deliriant in its effects, at least as they were shown in the film. I recall seeing a couple walk down the street, a few apart from one another, with a voiceover from the guy about how they communicated telepathically on it.
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Parkisan is a trihexiphenidil?or something like that.Antiparkinson drug.Never tried it,but its delleriant...even in small doses.Awful stuff,but there he has his own group of fans.Yes i heard that combo codeine and gluthed gives nod like H
 
Tramadol went from inactive to very active for me. Tried it during my oxy and heroin use with no effect hardly. Then one day in the midst of buprenorphine withdrawal when kratom and loperamide weren’t doing shit for me, I tried it again. Within an hour I was flying so high from 100mg. My theory is that either Bupe and tramadol share some receptor profile or my enzymes changed.

We know heroin oral bioavailability is much higher for dependent users than naive, so enzymes do change over time with these drugs I’m sure.

-GC
 
G_Chem said:
Tramadol went from inactive to very active for me. Tried it during my oxy and heroin use with no effect hardly. Then one day in the midst of buprenorphine withdrawal when kratom and loperamide weren’t doing shit for me, I tried it again. Within an hour I was flying so high from 100mg. My theory is that either Bupe and tramadol share some receptor profile or my enzymes changed.

We know heroin oral bioavailability is much higher for dependent users than naive, so enzymes do change over time with these drugs I’m sure.

-GC
Click to expand...
I experienced bupre & tramadol synergy during
w/drawal also
 
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