Alcohol Alcohol vs. Benzos. Which one is more euphoric/awesome?

[4DQSAR]

True but industries have had to deal with changes like this before and also, are you sure people wouldn't perhaps not drink that much less but use this more? For instance someone who drinks on average 5 beers a week but still drink 4 or 5 beers a week but also start using this on the nights they don't drink. What are the long term effects? It seems like a loss of brewing jobs would be worth the loss in negative health impacts of real alcohol.

Now of course we couldn't test the long-term effects and that was why my initial suggestion was that the compound be used for alcohol detoxification i.e. it's tested to the standard of any synthetic medicine and only then consider making it a licenced product - we though using the system in place that controls the sale and supply of alcohol i.e. tax and duty can be collected (KEY), kids cannot buy it nor can anyyone who is already clearly under the influence.

But that's where the problem arises. By the time it reached market, any patent would have expired UNLESS you were able first to obtain a patent based on it's use in alcohol detoxification and then a second patent as an alcohol alternative.

At the time we assumed it would be a 30 year project but we MAY live to see the benefits. Now, we would be unlikely to live to see any benefits although our various offspring DO hold details of the Supercats.

 

[Esperighanto]

Now of course we couldn't test the long-term effects and that was why my initial suggestion was that the compound be used for alcohol detoxification i.e. it's tested to the standard of any synthetic medicine and only then consider making it a licenced product - we though using the system in place that controls the sale and supply of alcohol i.e. tax and duty can be collected (KEY), kids cannot buy it nor can anyyone who is already clearly under the influence.

But that's where the problem arises. By the time it reached market, any patent would have expired UNLESS you were able first to obtain a patent based on it's use in alcohol detoxification and then a second patent as an alcohol alternative.

At the time we assumed it would be a 30 year project but we MAY live to see the benefits. Now, we would be unlikely to live to see any benefits although our various offspring DO hold details of the Supercats.

Vaguely off topic but it still relates to alcohol, you're somebody who obviously has a solid understanding of structure-activity relationships and you seem to have a solid grasp within the domain of sedatives as well. I'm curious, do you think that any other alcohols would ever take off commercially, assuming they were legalized? Methylpentynol, ethchlorvynol, 2M2B, GHB, chloralodol, trichloroethanol, and diethylpropanediol are all examples of different sedative alcohols, some very dangerous, some only a little bit less dangerous than ethanol, but do you think that any would ever take off assuming a big pharma company got them passed, and they were then sold in small and controlled doses?

I'm fascinated by ancient sedatives, piperidinediones like methyprylon and glutethimide, 1-Ethynylcyclohexanol (I usually just write it as 1-ECX), etc., this reddit thread I recently came across when Googling around for experience reports of 1-ECX has some interesting claims made surrounding various psychoactive alcohols.

 

[4DQSAR]

Vaguely off topic but it still relates to alcohol, you're somebody who obviously has a solid understanding of structure-activity relationships and you seem to have a solid grasp within the domain of sedatives as well. I'm curious, do you think that any other alcohols would ever take off commercially, assuming they were legalized? Methylpentynol, ethchlorvynol, 2M2B, GHB, chloralodol, trichloroethanol, and diethylpropanediol are all examples of different sedative alcohols, some very dangerous, some only a little bit less dangerous than ethanol, but do you think that any would ever take off assuming a big pharma company got them passed, and they were then sold in small and controlled doses?

I'm fascinated by ancient sedatives, piperidinediones like methyprylon and glutethimide, 1-Ethynylcyclohexanol (I usually just write it as 1-ECX), etc., this reddit thread I recently came across when Googling around for experience reports of 1-ECX has some interesting claims made surrounding various psychoactive alcohols.

OK all of those substitute unselectively enhance the action of GABA within the brain (or at least that is my understanding) while 1,4-benzodiazepines are selective to 5 suelective subreceptors of the GABA site. The first alcohol mimic was selective to just one subtype site, the Supercats to all three of the a5 subreceptors. As I said, Pyeyzolam emulates 'drunk' wonderfully but cannot emulate 'a glass of wine' for example. Hence the Supercats. We sold the Pyeyzolam patent to Nutt because we knew it was of no use... but we wanted a lot more for the Supercats. Not so much money but actual seats on the board because even Nutt's partner is essentially a scammer so we presumed any board would likewise be scammers.

 

[Esperighanto]

OK all of those substitute unselectively enhance the action of GABA within the brain (or at least that is my understanding) while 1,4-benzodiazepines are selective to 5 suelective subreceptors of the GABA site. The first alcohol mimic was selective to just one subtype site, the Supercats to all three of the a5 subreceptors. As I said, Pyeyzolam emulates 'drunk' wonderfully but cannot emulate 'a glass of wine' for example. Hence the Supercats. We sold the Pyeyzolam patent to Nutt because we knew it was of no use... but we wanted a lot more for the Supercats. Not so much money but actual seats on the board because even Nutt's partner is essentially a scammer so we presumed and board would likewise be scammers.

Thank you for the info here! Appreciate it.

 

[Smyth2]

Do you think Prenderol is a good alcohol?

There's a few of them. One like CGP-7930 looks interesting.

Another compound that looked quite interesting is called Ethyl acetoxy butanoate (EAB). I recommend you look into that if you want a ghb replacement.

 

[4DQSAR]

Prenedrol? Wasn't the (di)carbamate ester used medically and was somewhat more potent and long-acting? With all of those alcohols, the TI doesn't seem too great.

If for some crazy reason you saught a GHB alternative, HOCPCA would seem not only the safest but also the cheapest. I mean, that increased affinity isn't linear with the potency and if rather than grams, tens of milligrams is active, it's an entirely different business model.

Large-scale GHB production takes many people and large volumes of materials - the product itself being a saturated aqeous solution. Powder IS possible, but why bother? It's just not worth the effort.

IF you are intent on the simplest and best novel CNS depressant, 4-methyl pregabalin seems the better option once you understand how pregabalin is produced.

 

[Smyth2]

ok thanks for that i will add HOCPCA & 4-Methylpregabalin to my database later.

btw a carbamate is the same thing as a urethane but it is not an ester.

 

[4DQSAR]

ok thanks for that i will add HOCPCA to my database later.

It's also such an unusual structure, I doubt anyone would even check what it was. It really IS a useful solvent. It has the ability to solvate both lopophilic and hydrophobic compounds. I did wonder about it's practical usility as a solvent.

But when you see how pregabalin is produced, you will see why 4-methyl pregabalin isn't a stretch. Just change on (achiral) precursor to a chiral (but cheap) one. It's cheap as chips because it's waste from something else.

 

[Esperighanto]

Large-scale GHB production takes many people and large volumes of materials - the product itself being a saturated aqeous solution. Powder IS possible, but why bother? It's just not worth the effort.

I've witnessed GHB production on the scale of ~10 gallons before performed in the bedroom of a teenager, the only risk was the nitric acid fumes, he just had a bunch of box fans blowing out of an open window into the woods to handle that. I didn't stick around for long, the scent was absolutely heinous in there. Also for future readers, GHB in crystal form is overwhelmingly hygroscopic, meaning that it absorbs water from the atmosphere. In doing so, it gains an unknown amount of water, so you cannot then accurately dose your GHB, and with GHB having such an incredibly narrow therapeutic index, that can be very risky.

But when you see how pregabalin is produced, you will see why 4-methyl pregabalin isn't a stretch. Just change on (achiral) precursor to a chiral (but cheap) one. It's cheap as chips because it's waste from something else.

Quick question, but pregabalin production requires hydrogenation, yeah? I have always wondered if certain moieties don't survive hydrogenation well, just a generalized chem question, but if you had say, beta-methyl-phenethylamine, and you threw it in a hydrogenator, what resources would you advise I go to to research my hunch that it would end up as a mixture of para-hydroxy-beta-methyl-phenethylamine, N-hydroxy-beta-methyl-phenethylamine, and then each of those but with a beta hydroxyl group. I couldn't find much about this in Organic Chemistry As A Second Language, so I'd love it if you would just point me towards any textbooks or other resources where I could study mechanisms like this in greater detail.

 

[4DQSAR]

No - GHB production requires such vast volumes of quite nasty solvents and reagents to turn a profit, it's more like cookery than chemistry. Such huge scales and the associated fumes mean it's not a case of IF you will get caught, only WHEN you will get caught.

Since pregabalin is so widely used medically, there are constantly new routes designed to lower the bulk cost. Although once it reached $50-$100/Kg, surely further improvements would only pay off if you think you will use the 'latest' method for a long time?

But here is the thing. What if your company was an early adopter of a slightly more costly route? If you can only make it for $120/Kg, you suddenly have potentially millions of dollers of production-line sat idle. ANY company in that position would just love someone to ask for 4-methyl pregabalin for the truly HUGE price of, say, $400/Kg. The problem isn't cost, the problem is scale. Unless you want 100Kg and are prepared to enter into a contract promising you will buy a tonne per year, the numbers don't work.

But the very last thing you would do is make it yourself.

It's supposed to be subjectively identical to pregabalin based on human trials and 2-3 times as potent.

But I for one do not foresee myself sat with a large capping-line, blister-packing line and worst of all, the sucker who puts the strips into boxes along with the PIL. If you employ muppets, fine. But muppets are not to be trusted.

 

[Esperighanto]

No - GHB production requires such vast volumes of quite nasty solvents and reagents to turn a profit, it's more like cookery than chemistry. Such huge scales and the associated fumes mean it's not a case of IF you will get caught, only WHEN you will get caught.

Yeah this was not really a for-profit venture, some of it was sold but this kid was insanely physically dependent on it, I would explain further but it might delve too deep into synthesis talk for BL. The fumes were fucking terrible, we were in a rather rural area in a rainforest though and the humidity was causing huge problems, since this guy was not using inert atmosphere where he should've been.

But here is the thing. What if your company was an early adopter of a slightly more costly route? If you can only make it for $120/Kg, you suddenly have potentially millions of dollers of production-line sat idle. ANY company in that position would just love someone to ask for 4-methyl pregabalin for the truly HUGE price of, say, $400/Kg. The problem isn't cost, the problem is scale. Unless you want 100Kg and are prepared to enter into a contract promising you will buy a tonne per year, the numbers don't work.

The capitalistic analysis of this is really fascinating, I appreciate the insight here!

 

[pcplease]

I havent seen 4 methyl pregabalin available in several years, at least I think it's been around a decade since it first popped on my radar and 2017-2020 somewhat common.

Up until a couple years ago, pregabalin in sub <50g amounts was only a few dollars per gram, though, which to me seemed a small premium to pay for pregabalin's longer history of use.

 

[4DQSAR]

4-methyl pregabalin was patented in 2018 so I am surprised since although it uderwent human trials, it had no 'clinical advantage' over pregabalin. As with all such things - who knows what the mystery powder really is.

 

[pcplease]

my timeline might be a little off. i remember that it was patented, and i know it was still available through 2019 if not 2020. That said, the only two things that pop up on drugsdata.org are from 2022-2023 and what was sold as 4-methyl-pregabalin, one was simply pregabalin and the other a collection of unknown chems (noting that at that point, they had no reference sample for 4-methylpregabalin)

 

[4DQSAR]

Well it certainly coud have been 4-methyl pregabalin. Although not very potent, the extreme low cost and legal status would surely make it attractive to anyone looking to produce for what is actually a hugely expanding marker. But as I noted, I assume someone would produce samples at bench scale but that would cost thousands per gram, but maybe their was insufficnet interest at the time OR they couldn't work out how to find and obtain a contract with a legitimare pregabalin producer with spare capacity.

A scaling problem. Do you have sufficient faith in the product to sign an agreement to have tens of millions of units made. Just think of the logistics. You would need the entire cast of The Muppets capping and boxing and buyers worldwide. No easy task.

AFAIK outside the UK, it's still legal everywhere, but if you swamp a market, prices plunge.

 

[Smyth2]

Ethyl acetoxy butanoate (EAB)
[25560-91-2]

EAB is a colorless, transparent liquid with a fruity aroma. EAB is a good muscle relaxant, anesthetic and hypnotic. It is safer and more effective than traditional drugs for treating sleep disorders (such as barbiturates and γ-hydroxybutyrate). Patents such as US4,599,355 and Can.1,263,843 have described in detail the pharmacological effects of EAB and its similar compounds. It can be slowly hydrolyzed in the body to exert its efficacy, so it is safe and has a long-lasting efficacy. Large doses can have a continuous effect for more than 12 hours without poisoning. In addition, it has been found that EAB can inhibit the release of dopamine in the brain, so it is a potential drug for anti-Parkinson's disease, anti-schizophrenia and anti-psychotic.

Xiang Xiaoqing, et al. CN1047589 (1999 to Fudan University).

 

[vision conquest]

I'm sure it's already been mentioned or noticed here by people, but benzos don't bind to GABA receptors, they act as potentiators that essentially pretty pry the GABA receptors further open, if that makes sense. The pharmacology of GABA drugs is super nuanced and still isn't fully understood. Alcohol is also, as mentioned earlier, an incredibly messy drug as far as how it binds.

The description of a Venn diagram, with GHB on one side, benzos on the other, and alcohol in the middle is very applicable imo. Benzos are more "neatly drunk", and GHB is more "sloppy drunk", in this allegory (is allegory the right term here? I just woke up, sorry.)

Benzos have distinctly intense amnesia and delusions of sobriety, alcohol is perhaps the most toxic though. Keep in mind too that both vary, Jamaican rum vs cider vs vodka are so different, as are the majority of benzos from one another. In the is USA right now (the only area I'm familiar with) you're likely to encounter Bromazolam, Etizolam, Bromonordiazepam, Phenazolam aka Clobromazolam, Alprazolam, Clonazepam, Lorazepam, Diazepam, and each one is very unique, if you have questions about any of them feel free to ask away.

Benzos are positive allosteric modulators, which means, as you said they make the receptor more able to accept the action of gaba.

For me it's benzos anyday, and from my experience the ultimate benzo experience is alprazolam and diazepam together, I take the alprazolam first, let it kick in and then drop some diazepam, and it only has to be a conservative dose of diazepam, 2mg alprazolam and then 5-10mg diazepam, lovely combo.

I don't mind alcohol but in my opinion you need to work out how to best consume it for your body, a lot of bad experiences with alcohol are due to drinking too much to fast.

 

[Esperighanto]

4-methyl pregabalin was patented in 2018 so I am surprised since although it uderwent human trials, it had no 'clinical advantage' over pregabalin. As with all such things - who knows what the mystery powder really is.

I can't find the records of the conversation right now (I think they got autodeleted due the platform they were on) but I was talking to an analytical chemist who claimed that trying to identify 4-methylpregabalin was specifically a pain in the ass with the majority of techniques they were using, it was NMR and (either GC or LC)/MS, I can't recall many details about it but it seemed tricky to properly characterize on that level, and I wish I could recall more of that conversation. I sure do wonder if 4-Methylpregabalin would be potent enough to fit in gel tabs, even if they're double sized. I'm shocked that there's no experiential difference (beyond potency, ofc) as tolibut varies noticeably from floribut and phenibut even though I've only come across tolibut a handful of times at most.

Ethyl acetoxy butanoate (EAB)
[25560-91-2]

EAB is a colorless, transparent liquid with a fruity aroma. EAB is a good muscle relaxant, anesthetic and hypnotic. It is safer and more effective than traditional drugs for treating sleep disorders (such as barbiturates and γ-hydroxybutyrate). Patents such as US4,599,355 and Can.1,263,843 have described in detail the pharmacological effects of EAB and its similar compounds. It can be slowly hydrolyzed in the body to exert its efficacy, so it is safe and has a long-lasting efficacy. Large doses can have a continuous effect for more than 12 hours without poisoning. In addition, it has been found that EAB can inhibit the release of dopamine in the brain, so it is a potential drug for anti-Parkinson's disease, anti-schizophrenia and anti-psychotic.

Xiang Xiaoqing, et al. CN1047589 (1999 to Fudan University).

I've read of this Sodium 4-Hydroxyvalerate, EAB, MAB, and possibly T-HCA (Trans-4-Hydroxy-Crotonic Acid), GHV and DHV, and as a GHB enthusiast, I've always wanted to try them. Has anybody here ever sampled EAB, or any of these others?

 

[notsmokeymcpot42088]

Ethanol is just too damn harmful.

FUBAR you have tried the more euphoric benzos correct? Lol believe me I would toss my bottle out the window for a 5-10 mg dose of C-lam or F-lam. Which is a hefty dose but I would find it tough to believe (if you could remain awake) that it would not be more euphoric --- totally subjective I suppose hey.

sorry to interrupt the adult table lol

 

[4DQSAR]

Esters of GHB are simply GHB prodrugs thus if for some bizarre reason someone insist on going down that pathway, (R) HOCPCA is obviously the endpoint until and unless something of similar synthetic complexity but higher potency turns up. Since it's essentially a rigid analogue of GHB, I would presume that like pheibut, one could likely introduce an aromatic. But the LogP of (R) HOCPCA might mean such a substitution wouldn't increase activity by much.

But for me at least, GHB is only one step up from glue-sniffing.

OT when I lived in The Netherlands, I woke one morning and looked out of my window to see a dozen police vehicles in the street. It turned out that four police officers (two couples) had indulged in a sex party the night before, consumed GHB and other things and wound up dead.

I see one death as one too many. If you are producing GHB analogues, it comes with a death-toll.