GABAergic research chemicals

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I was just wondering what GABAergic RCs are out there besides benzos and 2m2b?

1,4-bdo, phenibut, tolibut, fluorophenibut, n ethyl zolpidem, zolpidic acid, pagoclone, 4-methyl-pregabalin (although this one might not be available, only seen it mentioned and not in the wild), quaalude analogs (mebroqualone, etaqualone, etc.), chloral hydrate and it’s derivatives, ether, various other alcohols may be recreational too, look in to fusel alcohols. There was also a simple chain carbamate based molecule on the market, would be similar to barbiturates but there are concerns about its safety. If you’re thinking about PM’ing for sources think twice.

I’m going to take this to basically mean non opiate sedatives.

I’d recommend 14BDO. It’s very easy to get your hands on, and as far as I can tell it’s reasonably safe with research, harm reduction, and moderation. Dosage is tricky IME.

Also have a lot of experience with phenibut. It’s truly a delight, but very psychologically addictive, and then physically addictive. The rebounds from even a few days of consecutive use are miserable.

1-2 g phenibut 2 hrs before drinking makes alcohol exponentially more euphoric. I take 2.5 g with 20 mg propranolol before public speaking for anxiety. Really helps. 1 g at bedtime greatly improves quality and length of sleep though it won’t knock you out if that’s what you need. Best of all it’s super cheap and 100% legal and can be bought with a credit card. It causes withdrawals if you take it everyday though. Wouldn’t recommend more than once a week.

Phenibut effects GABA but is actually a gabapentinoid.

Ignore the two comments above mine — you’re correct. Gabapentinoids are NOT GABAergics, they modulate voltage-gated calcium channels. Phenibut is unique in that it is a gabapentinoid that acts as a GABAb agonist in addition to its gabapentinoid properties.

All Gabapentinoids act on the calcium channels. (Gabapentin and Pregabalin). Meanwhile, only GHB/GBL/BDO acts on the “GHB receptor”, even if Phenibut and Baclofen cause some euphoria as well…

why for then does Wikipedia define gabaergic as: “A GABAergic agent or drug is a chemical that functions to directly modulate the GABA system in the body or brain. Classes include GABA receptor agonists, GABA receptor antagonists, and GABA reuptake inhibitors. Examples of types include gabapentinoids and GABA analogues.”

Are you implying Wikipedia is a reliable resource? By this logic, only phenibut falls under one of those listed classes (GABA receptor agonists).

The Wikipedia pages for gabapentin, pregabalin, and even the page for gabapentinoids in general explicitly state that they are not GABAergic…

Phenibut is a Gaba B agonist, similar to GHB/GBL/BDO, Gabapentin, Pregabalin and Baclofen.

GABAergic substances are all substances that agonize GABA A and B receptors. But quite frankly, GABA A agonists are really dangerous and not as entertaining as GABA B agonists.

Benzos, Barbiturates and Alcohol are among the most addictive and life threatening drugs out there. GHB/GBL is very addictive, but the amount of damage it causes is virtually inexistent. Some neurotoxicity occurs when you’re not responsible and pass out frequently during the day, in public…

Gabapentin or pregabalin don’t touch gaba b though that’s what makes phenibut a different type of gabapentinoid.

Aren’t barbiturates GABA-B? And way more deadly/dangerous than benzos. It’s not about which receptor site it hits, it is about how it modulates the receptor. Benzos increase the frequency at which the receptor will accept GABA. Barbiturates increase the duration that the receptor will accept GABA for. Too much duration and you’re dead, but even at high frequency, you won’t die because there’s still time in which it is not activated. Obviously this is ELI5.

At least that’s my understanding. It’s been over 5 years since I read into it much.

Barbiturates are Gaba A agonists. They might agonize Gaba B a little but most of their effect is caused by Gaba A.

Duration has no importance towards potency and danger. Phenibut lasts for 12-24 hours, maybe even more, but it’s perfectly safe. GHB/GBL on the other hand, lasts for 1-2 hours, but it’s still pretty safe physically and psychologically if treated with respect. Just like with LSD, people might fall on sharp objects and get hurt, but overdoses are virtually unheard of and all the people that have died because of GHB (without co-intoxicants) had cardiovascular problems and experienced cardiac arrests.

Strangely enough, even if GHB/GBL is extremely sedating when you take 20% – 50% more than your habitual dose, respiratory arrest and failure is also incredibly rare, if not impossible. Barbiturates, Benzos, Alcohol and Opiates are known for their harsh and long overdoses, which often cause respiratory arrests and death if no one is there to help. I’ve made countless posts and replies about this incredible “defense mechanism” GHB/GBL creates to protect the person from dosing again or the brain and body from destroying itself. You can drink 20-30 times the habitual dose (1gr/1ml) and just pass out, sleeping like a baby for a few hours, without any breathing problems or vomiting while in this state.

Ok that is great for GHB, but benzos are the same when used on their own.

My explanation for the difference between barbiturates and benzos wasn’t discussing duration of effect, it was discussing the way in which barbiturates effect the GABA receptors and what makes them more dangerous than benzos. Frequency vs duration of the GABA receptor (or its ion channel) being open. Wiki will explain better: Barbiturates produce their pharmacological effects by increasing the duration of chloride ion channel opening at the GABAAreceptor (pharmacodynamics: This increases the efficacy of GABA), whereas benzodiazepines increase the frequency of the chloride ion channel opening at the GABAA receptor (pharmacodynamics: This increases the potency of GABA). The direct gating or opening of the chloride ion channel is the reason for the increased toxicity of barbiturates compared to benzodiazepines in overdose.

So yeah, they are GABA-A, confirmed that on wiki too, but so are benzos, and benzos are just as safe as GHB when too many are taken. The reason for safety is a lot more complex than GABA-A vs GABA-B like you assert.

I’m not a pharmacologist, and I was just trying to explain the difference in a simple way. Barbiturates are way more dangerous than Benzos, but Benzos are as dangerous and toxic as Alcohol. Respiratory arrest and Cardiac arrest are frequent in overdoses, and their most vicious ability is addiction. Benzos and Alcohol are the only substances that can cause lethal withdrawals and quitting them cold turkey is always discouraged by doctors. This obviously depends on length of use and amount used during the addiction, but none of this happens with Gaba B agonists.

They work differently and their effects are way more subtle physiologically. I don’t know if I’m making any sense, but Gaba B agonists will basically shut down your brain, Gaba A agonists will shutdown your entire body during an overdose. That’s what makes them dangerous in the first place.

The main source of such statements is my experience with them, but differently than most people, I’ve passed entire nights reading about the pharmacology and psychological effects of psychoactives, from Alcohol to DMT. It’s been a few years since I stopped reading and eating through articles and studies, but I must admit, I was never much into Alcohol, Benzos and Opiates/Opioids, hence I lack the necessary knowledge to fully explain how they work. Thanks for your reply, you had really interesting info there

Fair point about the withdrawals for benzos, but I must say they are far less dangerous for acute overdose (respiratory depression and death) than alcohol. Alcohol alone will kill someone at maybe 4x the dose to get drunk. For benzos you’re looking at 20 (for the anesthetic kinds like midazolam and triazolam) – 50x (Xanax) an effective high dose, or even 100s x for some like clonazepam.

Benzos are very dangerous in combination with other depressants, but on their own they are very safe.

Good convo man, thank you for your perspective on them, it is a good overall explanation I do agree now that GABA-B agonists seem safer overall now that I think about it. GHB, baclofen and phenibut (I think?), any others that are common? These are all very safe compared to benzos barbs and alcohol.

Here in Canada we have carisoprodol / Soma. It’s good stuff, but AFAIK a Canada only loophole.

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