Gaboxadol

[Hammilton]

I'm going to be giving gaboxadol a trial soonish, just waiting on it Will document it here / erowid, of course.

Anyway: it's described by Lundbeck / Merck (iirc) as having a "shallow benefit to risk ratio" -- which I assume is the psychiatric effects that begin around 20-25mg (again, IIRC). Since it made it's way pretty far, it's not obviously toxic, but a. were any deaths associated with it's trial and b. what exactly was the LD50, if only in mice, it'd be beneficial.

Any info about time to onset, length, etc in humans? mice? Ie: if I take 10 or 15mg, how long do I have before I become sedated?

I don't see disinhibition listed as a side effect. Is it?

 

[bob_arctor]

Very interesting - followed this one until it limped out of the race, good to hear that the potential potential is potentially potentialled out. Looking forward to hearing more.

 

[Hammilton]

It's definitely going to be "potentialed out" but I'm pretty nervous, to tell you the truth. I may not be the first person to taste it, but quite possibly the first outside of research studies.

I don't see it appearing on the RC market. The synthesis is quite difficult.

Interestingly, the Merck page on why it was discontinued says "Schedule IV." I assume that they talked to the DEA or something to see what they'd Schedule it because I find no record of it actually being scheduled.

 

[Sturnam]

Hey, I found some stuff for you.

It has an elimination half-life of 1.5–2 h and maximal plasma levels are reached within 30 min after oral administration...
In humans, comparable observations have been made. In young healthy men, a single oral dose of 20 mg gaboxadol was found to increase sleep efficiency, to promote slow wave sleep and enhance the slow frequency components in the EEG within non-REM sleep...

Also notes multiple times that the participants (old people) had absolutely no side effects, and no impairment the next day.

from: Effect of Repeated Gaboxadol Administration on Night Sleep and Next-Day Performance in Healthy Elderly Subjects
Neuropsychopharmacology (2005) 30, 833–841

 

[MurphyClox]

The following data should be taken with some care, as it was directly derived from a patent. Inventor and applicant was Povl Kroogsgard-Larsen, now employed at the Faculty of Pharmaceutical Sciences of the University of Copenhagen (see: EP 0 000 338 A2 (1979)).

- Binding affinity in vitro performed according to Brain Res 1975, 100, p.81 (given are the concentrations that lead to 50 % inhibition of GABA-binding):
Gaboxadol = 0.13 ± 0.005 µM
Muscimol (for comparison) = 0.024 ± 0.003 µM

- Acute toxicity (given are LD50-values in mg per kg bodyweight):
Gaboxadol i.v. = 80
Gaboxadol i.p. = 145
Gaboxadol p.o. = >320
Muscimol i.v. = 7
Muscimol i.p. = 12
Muscimol p.o. = 22

Recommended dosage: 15 mg for adults, 5-10 mg for elderly (info taken from a publications by the Lundbeck company)

No idea about duration of onset or over-all duration of effects. This has to be assayed, I guess.

Peace! Murphy

 

[Cwest]

any new info on this one?

 

[Solipsis]

I just hope you have verified that it is in fact gaboxadol and not ibotenic acid like I received instead of gaboxadol.

Still a little jaded about that as well as interested in converting it (if I hadn't lost the friggin stuff ), maybe a report of yours can cheer me up... speaking of hypnotic effects readily occurring followed by lucid amanita muscaria like dreams and a refreshed waking.

 

[Poelster]

Did this compound ever got samples by anyone here?

And Sturnam, where did you found this information?

I've been reading some of the Lundbeck publications as well, and the most common dose I see reported is 5-10mg, like Murphy found. Altough in one of the patents they claim a dose of 20-25 is most beneficial.

Soon, I'll be receiving my sample and if nobody as sampled it here before, I'll start with 5mg, just to be on the safe side.

And I presume that this compound gets transported into the brain (because zwitterions don't really diffuse that well ). Does anyone know which transporter is involved, as in possible DDI?

 

[Poelster]

As said, I started with 5mg, after it was confirmed to be genuine gaboxadol.

This didn't do much for me, I did felt slightly intoxicated, but nothing noteworthy.

Last night I tried 10mg. A couple things stood out. It felt totally different then any other GABAerigic compound I've tried. It had a distinct and pronounced body-high, much more so then a mental high. I had no trouble staying up and staying focussed, I just felt super relaxed. Motor skills were inhibited.
After I went to bed, ~3h after taking it, I noticed the mental component. It's not as drowsy as benzo's, it's more dreamy in it's nature, if that makes sense.

Sleep was good and deep, Woke up once during the night and was surprised to find out I still had a couple more hours. Going back to sleep was no problem, although I did already feel completely rested.
No drowsiness the next morning, which I think, is so far the biggest plus for this compound!

But by all standards this dose didn't felt strong, next time will be 20mg. And then I'll see if this compound has more to offer.

Someone also told me that it doesn't work as well if one were to use it right after a meal that contained a lot of protein, i.e. meat, likely due to some competition for some amino acid transporters?

 

[Incunabula]

According to this article, 35 mg is needed to feel anything more than sleepiness.
http://harpers.org/archive/2013/08/gaboxadol/5/

Would love to try this one. Maybe it''ll find me some day
How did you aquire it, btw? (not sourcing here, guys!!!) Just curious if it was from a research chemical vendor? custom synth? Personal contact in the pharmaceutical industry? etc..

 

[Poelster]

Thanks for the article, was a nice read.
Although it's weird that he thought it was ibotenic acid, because there's no way the two could be confused. And I don't think this compound is that suitable for GC analysis, because it was most likely as the (HCl) salt.

I got it from a friend who had it laying around for some time, but never had tried it. So with the analysis that was done, we proved that it not only was the correct compound, but can easily be stored, without the need for putting it in the frigde, etc.

More experimenting will soon follow.

 

[Incunabula]

Cool, thanks. Keep us updated

 

[Poelster]

Had two more trails with this, both 20mg.

The first 20mg, I also had smoked some weed, which, as it turned out, had some serious synergistic effect. All I could do was just lay on my couch and be somewhere between reality and a vivid dream world. It was strange but pleasant, and above all unexpected.
Two days later, tried it again and decided to stay on the same dose, but without anything in combination. To see how much was caused by this compound alone. As it turned out, this time, it was way milder. Just an enhancement of the effects that I got at 10mg.

 

[Poelster]

At the dose range of 50mg this compound starts to have additional effects. It felt in some way similar to a low dose of ketamine, but where ketamine is more quiet, this compound produced a more nervous-kinda state of mind. Images apparent in my mind, they really felt like memories. That was the strange thing, but they were of bizarre and absurd situations that could/would never happen, but they were life like nonetheless. As quickly as a image appeared, as quickly it disappeared and the next one would pop-up. This flashing of images was what caused the nervous feel. It wasn't unpleasant, but can't really call it pleasant either. Another interesting point was that I now actually had trouble getting to sleep, but once I finally did I fell into a deep sleep. The next morning there was a slight hangover, something I also had experienced with 40mg, but then there were no dissociative effects.

Also tried 60mg, and those effects were similar to those of 50mg.

Have now also more experience at the lower dose ranges. 20-30mg is the ideal dose for me, as a sleeping agent. And in all aspects it's superior to benzodiazepines. It's such a shame this never reached the market.

I also think it's interesting that this compound hardly tastes of anything, even at the 60mg dose. When dissolved in a glass of tapwater, only a slight bitter taste occurs.

 

[Ligaturd]

I believe I read of Muscarinic drugs actually being able to increase sleep quality which most sleep medications don't (except for Mirtazepine and Temazepam if I remember correctly) I guess none of them are making it past phase 3 trials due to their effects? Exploration into muscimol analogs would be interesting as well for other purposes. It's a shame. I would love to see more being investigated.

 

[Incunabula]

I recently talked to a guy who's on the inside of a pharma company. He knew a guy who had taken a smallish dose for sleeping, and had then had a seizure. The person was young and healthy and had no prior history of epilepsy. I know it's a complete second hand anecdote, but it might be one of the reasons this wonder sleeping tablet never got marketed.

I'd still like to try it though.

 

[Poelster]

The quality of sleep is definitely improved with this compound. The problem is that all other analogues, like thio-thip, aza-thip etc are inactive at the same extrasynaptic GABAa receptor. Also methylating the nitrogen or extension of the ring size doesn't work, so basically gaboxadol is a one of a kind, unfortunately.

Several of my friends have also tried it, one of them actually having a recent history of epileptic attacks, but none experienced any side effects. As far as I know he didn't go above the 25mg dose, though.