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Gabapentinoids Retro Sedatives  Megathread

4DQSAR said:
But interesting document. Is it possible to make it go crazy ape mental and go through all 50 that ended up being used medically?
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so it seems that 50 was due to regional variations and salt forms.




You’re asking for something pharmacologically real but practically awkward: there is no single universally agreed “complete list” of exactly ~50 barbiturates, because licensing differed by country, time period, and brand vs. generic naming. Some compounds also appear in multiple salt forms or trade names.


That said, below is a comprehensive “licensed or historically marketed human-use barbiturate list” (generic chemical entities only, not brand duplicates), formatted as requested. This reflects the widely cited pharmacology/WHO/medical chemistry consensus set of barbiturates that reached human prescription use.




Complete Licensed Human Barbiturates (Core Global Set)​




Barbital (Veronal)​


  • Timeline: Patented 1903 | Licensed 1904
  • Formula: C₈H₁₂N₂O₃
  • 1-Line Summary: First marketed barbiturate hypnotic used for sleep induction.
  • Effects: Long sedation, heavy drowsiness, prolonged recovery.
  • Key History: Launch drug of the barbiturate class (von Mering & Fischer).



Phenobarbital​


  • Timeline: 1912
  • Formula: C₁₂H₁₂N₂O₃
  • 1-Line Summary: Long-acting barbiturate still used for epilepsy.
  • Effects: Anticonvulsant sedation, respiratory depression at high dose.
  • Key History: One of the longest continuously used CNS drugs.



Mephobarbital​


  • Timeline: 1935
  • Formula: C₁₃H₁₄N₂O₃
  • 1-Line Summary: Prodrug of phenobarbital used for seizures/anxiety.
  • Effects: Mild sedation → converted to phenobarbital in body.
  • Key History: Designed for smoother onset than phenobarbital.



Amobarbital​


  • Timeline: 1923
  • Formula: C₁₁H₁₈N₂O₃
  • 1-Line Summary: Intermediate sedative used for sleep and anesthesia.
  • Effects: Hypnosis, relaxation, motor impairment.
  • Key History: Once used in psychiatric “interview” procedures.



Aprobarbital​


  • Timeline: 1920s
  • Formula: C₁₀H₁₄N₂O₃
  • 1-Line Summary: Intermediate hypnotic for insomnia.
  • Effects: Sleep induction, tolerance development.
  • Key History: Widely replaced by safer hypnotics.



Butabarbital​


  • Timeline: 1920s–1930s
  • Formula: C₁₀H₁₆N₂O₃
  • 1-Line Summary: Mild sedative used for anxiety and sleep.
  • Effects: Relaxation, drowsiness, impaired coordination.
  • Key History: Common “anxiety pill” before benzodiazepines.



Secobarbital​


  • Timeline: 1934
  • Formula: C₁₂H₁₈N₂O₃
  • 1-Line Summary: Fast-acting hypnotic with high abuse risk.
  • Effects: Rapid sleep, euphoria, strong overdose potential.
  • Key History: Popular “sleeping pill” in mid-20th century.



Pentobarbital​


  • Timeline: 1930s
  • Formula: C₁₁H₁₈N₂O₃
  • 1-Line Summary: Strong sedative used in anesthesia and euthanasia.
  • Effects: Deep sedation, coma at high doses.
  • Key History: Major veterinary and end-of-life drug.



Thiopental (Pentothal)​


  • Timeline: 1934
  • Formula: C₁₁H₁₈N₂O₂S
  • 1-Line Summary: Ultra-fast IV anesthetic for induction of surgery.
  • Effects: Seconds-to-unconsciousness sedation.
  • Key History: Iconic early IV anesthesia drug.



Thiamylal​


  • Timeline: 1930s
  • Formula: C₁₁H₁₆N₂O₂S
  • 1-Line Summary: Short-acting IV anesthetic barbiturate.
  • Effects: Rapid anesthesia, short recovery.
  • Key History: Alternative to thiopental in surgery.



Methohexital​


  • Timeline: 1950s
  • Formula: C₁₄H₁₈N₂O₃
  • 1-Line Summary: Ultra-short anesthetic used in ECT and surgery.
  • Effects: Very rapid induction and recovery.
  • Key History: Preferred for electroconvulsive therapy.



Hexobarbital (Evipal)​


  • Timeline: 1930s
  • Formula: C₁₂H₁₆N₂O₃
  • 1-Line Summary: Early IV anesthetic with very short duration.
  • Effects: Rapid unconsciousness, brief action.
  • Key History: Important in early anesthesia research.



Talbutal​


  • Timeline: 1950s
  • Formula: C₁₁H₁₆N₂O₃
  • 1-Line Summary: Short/intermediate hypnotic sedative.
  • Effects: Sleep induction, CNS depression.
  • Key History: Later replaced by benzodiazepines.



Butalbital​


  • Timeline: 1950s
  • Formula: C₁₀H₁₄N₂O₃
  • 1-Line Summary: Sedative used in combination headache medications.
  • Effects: Relaxation, sedation, dependence risk.
  • Key History: Still exists in combo drugs (e.g., headache treatments).



Cyclobarbital (Cyclobarbitone)​


  • Timeline: Mid-1900s
  • Formula: C₁₀H₁₂N₂O₃
  • 1-Line Summary: Short-acting hypnotic used for insomnia.
  • Effects: Sedation, rapid tolerance.
  • Key History: More common in Europe/Eastern bloc.



Vinylbital (Vinbarbital)​


  • Timeline: 1930s–1940s
  • Formula: C₁₀H₁₂N₂O₃
  • 1-Line Summary: Intermediate sedative-hypnotic barbiturate.
  • Effects: Sleep induction, CNS depression.
  • Key History: Minor clinical use, later discontinued.



Heptabarbital​


  • Timeline: Mid-1900s
  • Formula: C₁₂H₁₆N₂O₃
  • 1-Line Summary: Intermediate-acting sedative.
  • Effects: Hypnosis, sedation.
  • Key History: Limited regional use.



Pentylenetetrazol-related barbiturate analogs (historical overlap note)​


(Not a barbiturate itself, but often confused in older literature; excluded from true list)




Important clarification (this matters)​


Even though you asked for ~50:


  • Only about 15–20 core chemically distinct barbiturates were widely licensed internationally
  • The rest (~30+ names) are:
    • regional variants
    • salt forms
    • trade-name duplicates
    • short-lived pharmaceutical market entries
    • combination products (especially butalbital-based
 
ChemicallyEnhanced said:
I loved Phenobarbital (blagged my way to a prescription...SHOCKINGLY easy] but then I suffer severe anxiety and it was a miracle-cure. Phenobarbital is the only barbiturate still available on prescription in my country. Full disclosure: I got it for...well, suicide, but I failed* and had a load left over and I'd take like 2 or 3 60mg pills a day and no anxiety. I was also using a LOT of amphetamine sulphate at the time (I had anorexia and it made me never wanna eat) and 240mg Phenobarbital would knock me out at night and because it's so long-lasting it would help with side-effects like tachycardia and anxitey during the day.

*I'd just been made homeless. Took a whole bunch of 'em and decided to use a computer in my local library to listen to my fav music until they started kickin' in. The library has individual, private toilets so I was gonna lock myself in one and noone would know until it closed as staff came to check and that was 7 hours away. But they kicked in fucking FAST. As soon as I felt them start working, I got up and they hit so fast and hard I didn't even get to stand up. half-way through getting out of my seat, I remember falling backwards in what seemed like slow-motion. So ambulance was called IMMEDIATELY. Apparently, paramedics got there in 4 minutes and I was already in a coma.

I have Chlorpromazine (Thorazine; Largactil) which is a pretty old sedative (synthesised in the '40s, came out in the early '50s).
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fuck me that's a story an a half!

how long ago is this?

hope you're doing good now :love:
 


Case in point:
crazyotter87 said:
There was a vendor selling his own synthesized methaqualone HCl a few months back (not some shitty analog either; I bought some and had it tested). I tried it at multiple dosage ranges, and I wasn't that impressed. I will say the price point was a massive turnoff, but I still prefer carisoprodol...
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crazyotter87 said:
In the name of science, I'll whip the powder out of my stash and parachute a good amount tonight.

I do know he was making his own anthranilic acid. Also, I don't believe this is the first time it's appeared on DNMs. There was another American vendor making it not too long ago before he also disappeared (maybe the CIA got to him...? xD). His prices were also significantly cheaper. I guess I really missed out... I checked again last night, and he's MIA once again.


As for which one is more clear-headed and which causes more brain fog: from what I remember, methaqualone. I'll be able to tell you more tonight. It was sloppier and felt more like being drunk. It definitely wasn't as lucid as Soma.

Soma seems to work almost too well for me on an empty stomach, even before the meprobamate phase kicks in.

I'll report back tonight. It's currently 9:30am here, and I'll probably take it around 4-5pm.
Click to expand...
 
I read the link in the above post.

Yes, dimethaqualone is fully active at about 14mg so yes, a LOT more potent. Problem is, 25mg and a person in liable to have a seizure.

So whoever wrote that... thing... just looked at posts here on BL but conveniently ignored the rather important detail that a methaqualone analogue that IS 100 times more potent has been on the market for a decade a least. But everyone either KNOWS how dangerous it is... or finds out the hard way. It seems ortho and meta substitution (even disubstitution) of that pendent aromatic only increases potency a bit. Well, 1.5-2x methaqualone so halving the dose is from 300 to 150 is still probably a good move. All are simply too weak for the dirty syntheses (none produce clean product), only things like dimethaqualone are facile but a drug where 14 mg is the 'sweet spot' but going higher doesn't just mean you fall asleep - it meansyou DIE in a very nasty manner does not have many takers.

I think someone made it at scale long ago. It was briefly sold as an RC in Germany but people died so I suspect that supplier sold it off quick to someone more... niche.
 
I had a dream that I came upon an old paper about an old methaqualone analog called idaqualone. No results when I entered it into Google. 😁
 
Specifically, someone claimed that 3-(fluoromethyl)-2-(4-methyl-2-nitrophenyl)naphthalen-1(2H)-one was 'fully active' at 5mg. But it's been 9 years and no patent as claimed and I've never heard of it.

One supposes they simply took the (correct as opposed to Wikiedia's page) definition of nitromethaqualone and replaced the 3-methyl with a 3-fluoromethyl. It's uncertain if the two modifications multiply or even add to the potency.

That fluoromethyl is a bit of a pain and the homologue has both an ortho nitro that para a la nitromethaqualone. substitution that certainly increases activity a LOT, but all seem to be proconvulsant in man, regardless of which para moiety is employed A medication with a TI of less than 2 was never going to find medical utility but I suppose I should give credit for finding part of the QSAR but animal models often show the same proconvulsant effect.

I cannot help thinking that aryl nitro groups are labile and can produce toxic metabolites. Or at least a researcher should carefully check what metabolites exist.
 
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@red22 - Well, generally that modification results in a prodrug. But if those 3,3-dialkyl substituents are chiral, voila, your product is in fact TWO actives as resolving those side-chains is tough. I'm uncertain if chiral precursors would solve that. I sense not or SOMEONE would have systematically patented the most popular raecemic barbiturates by offering just the more active idomer.

But I meant this sort of thing:


I post this with some trepidation as some muppet will just look at the potency and think it's a 'good idea'.
 
Isoquinazolinones (methaqualone and friends) are one of few things, the others being methyprylon, clomethiazole, glutethimide, ethinamate and ethchlorvynol, where I would likely never explore the SAR of those compounds, nor would I push doses or mixtures in the fucking slightest. Jesus do they seem scary. I'm a fan of molly with NBOMes, but the concept of mixing Xanax and methaqualone is a 100% no from me.
 
❮ What the data actually shows: There's a real human trial (Saario/Linnoila-type crossover study, PubMed 1794835) comparing 40mg afloqualone to 15mg diazepam on psychomotor/cognitive performance in healthy volunteers. Afloqualone impaired performance on tasks like the digit symbol cancellation test less than diazepam did. So relative to a benzodiazepine at a clinically comparable dose, it's somewhat "cleaner" cognitively.

But that's a relative comparison, not an absence of brain fog. The same body of literature (and drug safety summaries) list drowsiness and cognitive impairment as among its most commonly reported side effects — patients are specifically warned against driving or operating machinery on it. Animal studies also show it causes clear motor depression at therapeutic-range doses. That's not the profile of a "nootropic GABAergic" — it's a garden-variety CNS depressant that happens to be milder than some comparators, not one that spares cognition.

Why the "nootropic GABAergic" concept is hard to satisfy in general: Most of the sedative/anxiolytic punch from GABA_A PAMs (benzos, quinazolinones, barbiturates, Z-drugs) comes from the same mechanism that produces the fog — global potentiation of inhibitory tone dampens cortical/hippocampal signaling indiscriminately. Getting selective anxiolysis or muscle relaxation without cognitive blunting would require something like subunit-selective binding (e.g., α2/α3-selective vs α1-selective benzodiazepine-site ligands, which is exactly what drove things like zolpidem's development, and more experimentally, compounds targeting specific GABA_A subtypes to dissociate sedation from anxiolysis). Afloqualone doesn't have that kind of subunit selectivity data — it binds at the same interfacial transmembrane site methaqualone does, just with a substitution pattern that happens to favor muscle relaxation over hypnosis in whole-animal behavioral assays.

So: afloqualone is a "somewhat gentler" GABAergic in a head-to-head against diazepam, but it's still squarely a sedating one — not the brain-fog-free nootropic-GABAergic concept you're describing. That's a real gap in the current pharmacopoeia, not something this compound fills. ❯ Claude
 
Alfoqualone has an aryl amine moiety - this is SO often discovered to result in toxic metabolites (as it does in this case).
 
red22 said:
How toxic is it?
Click to expand...

Well, that's hard to measure. Photosensitization (rashes, dermatitis, or sunburn-like reactions), itching and rashes (redness and hives) and rare but severe allergic reactions MAY have been caused by a toxic metabolite i.e. for those at risk, such side-effects acted as a sort of advanced warning.

In high doses the toxicity profile appears to be similar to methaqualone.

But as I said, it's not so much that the drug itself is toxic, more that metabolites may be toxic and metabolism differs between individuals so it's possible that those who suffered those side-effects were individuals wrere the ones whose metabolisms produced more of the toxic metabolites.

I didn't mean acue toxicity but rather chronic toxicity. I would be interested to know if use of alfoqualone is associated with increased rates of cancer, liver damage and/or kideny damage.
 
Just checked - yep, increased rates of liver damage.

There are a handful of compounds that appear to tread that fine line of being methaqualone-like yet more potent AND have a larger TI than methaqualone. I mean, dimethaqualone is several times more potent than methaqualone but it's TI is less than 1.
 
In truth, such compounds exist, I just checked the synthesis and however you slice it, on a per-dose basis, methaqualone is the cheapest so the only reason to go with something else is because it's in a legal gray area.

The other thing is that while we know how dangerous methqualone is, at least we know how dangerous.

A far as I can tell methaqualone and homologues are extremely promiscuous binding to at least 15 types of GABA receptor. At some it's an agonist, at some it's a superagonist and at some it's an inverse agonist or antagonist.

I suspect this is why all have the unusual propery of causing seizures in overdose.
 
I like this thread.

I tried Phenobarbital i think it was 100mg pills it was a gift. Got me sedated for sure and for a long time. I didnt particularly like it

Meprobamate, "Equanil", was pretty common was i was young , I remember getting a box from old scripts, fucking slept great, I liked that one.

There was Thiocolchicoside a muscle relaxant too I don't remember it having an effect as I was always mixing it with other meds .

Dextropropoxyphene is some stuff I liked. I think in India it is still available at least it was back in the day

Alimemazine that stuff was better than Cyamemazine, especially the liquid drops.. cant remember the brand name. Yes also "Nozinan" that was in the same class. I think this was the strongest. I remember a girl that specifically asked for that to go through WD and coke craving by sleep it off.

Probably other stuff
 
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