HA-966

[negrogesic]

HA-966 is an NMDA antagonist/low efficacy partial agonist at the glycine site, and has recently become available for purchase. It apparently has anxiolytic, hypnotic and analgesic properties.

By appearance it is a sort of cyclized gaba analog, quite reminiscent of GBL but has not been characterized to behave as such. Any idea as to how it functions as a hypnotic? One notion I came across regarding the source of its hypnotic effects relates to a possible disruption of striatal dopamine (in the manner of GBL).

What is unclear is the duration of effects and dosing but I might give it a try anyhow.

 

[vecktor]

View attachment 19999

HA-966 is an NMDA antagonist/low efficacy partial agonist at the glycine site, and has recently become available for purchase. It apparently has anxiolytic, hypnotic and analgesic properties.

By appearance it is a sort of cyclized gaba analog, quite reminiscent of GBL but has not been characterized to behave as such. Any idea as to how it functions as a hypnotic? One notion I came across regarding the source of its hypnotic effects relates to a possible disruption of striatal dopamine (in the manner of GBL).

What is unclear is the duration of effects and dosing but I might give it a try anyhow.

the two possible enantiomers have different effects, one the R enantiomer is a glycine site partial agonist where it acts as a NMDA blocker the other enantiomer the S enantiomer causes muscle relaxation and sedation and possibly interacts with the GHB receptor. However GHB itself does not have sedative effects due to its interaction with the GHB receptor, the GHB receptor is responsible for the paradoxical stimulant effects of GHB.
The racemate itself is quite interesting, The individual enantiomers more so. the R produces anxiolytic effects without sedation or interaction with alcohol. The S enantiomer is pretty much unknown as the sedation ataxia and other effects meant pharma left it alone but actually it is probably the most interesting enantiomer.

Given both enantiomers have a zinc binding motif it almost certainly also interacts with other systems and probably has a rich and complex pharmacology.

 

[negrogesic]

The racemate itself is quite interesting

"Interesting" in the sense that you found it interesting from first hand experience, or interesting conceptually? The item for sale is the racemate.

I'm curious to trial it but dosing seems to be a gray area. Not sure of the pharmacokinetics either. Can't imagine it would be particularly potent based on that structure (and potency of relative compounds) but who knows.

 

[checktest]

Vecktor definitely is right- it has to have more interactions than just weak partial agonism of the NMDA glycine site. I wonder if it interacts with glycine receptors or transporters like ethanol may (especially the s enantiomer of ha-966) or some other relevant glycinergic mechanism.

The Glycine Receptor-A Functionally Important Primary Brain Target of Ethanol - PubMed

Identification of ethanol's (EtOH) primary molecular brain targets and determination of their functional role is an ongoing, important quest. Pentameric ligand-gated ion channels, that is, the nicotinic acetylcholine receptor, the γ-aminobutyric acid type A receptor, the...

www.ncbi.nlm.nih.gov

Reminded me somewhat of some of the racetams like the anticonvulsant leveracetam, but it is fairly different in motifs. SV2A receptor.

 

[polymath]

By appearance it is a sort of cyclized gaba analog, quite reminiscent of GBL but has not been characterized to behave as such. Any idea as to how it functions as a hypnotic? One notion I came across regarding the source of its hypnotic effects relates to a possible disruption of striatal dopamine (in the manner of GBL).

If it's not because of glycine, GABA-A or GABA-B receptor binding, then it would have to be an adenosine or alpha-2-adrenergic agonist or H1 blocker.

The sedative-hypnotic glutethimide is also a cyclic amide like HA-966, so this compound could even affect the GABA-A receptor in some similar non-benzodiazepine like way.

 

[negrogesic]

This is interesting. Apparently it induced EEG sleep patterns in monkeys while awake.

Anyone game to find out if HA-966 can induce a waking near death experiences as speculated here?

 

[negrogesic]

Update, I've taken up to 12mg with no effect, though I might have felt something with that last 12mg (i had already had a bottle of wine and 4g of phenibut at that point to it was hard to discern if it was doing anything).

Will try higher doses again during the day, though its hard to find time for that sort of goofing off (particularly if it is substantially inebriating).

Anyone have an intuition as to a dosing regimen for this stuff? It was sold quite inexpensively in lots of 250mg, thats about all i know (beyond the ostensibly large doses that were pumped into animals).

 

[Working_Class]

I've seen this stuff for sale at an insane price. The cost alone is the #1 deterrent for me, but keep us updated on if you can find a use for it or a proper dosing scheme. You're the only bluelighter I know of doing trials with this one.

 

[negrogesic]

Given its micromolar affinities it may be that high doses are necessary. I don't mind being a bit of a guinea pig but this quite an extreme case seeing i haven't found a single report of its consumption by a human.

 

[vecktor]

YMMV with all of this, as it depends on your weight and tolerance, this is from memory a long time ago.

76kg
Racemate 20mg = 1-2 units alcohol equivalent, fairly linear dose response up to around 160mg which is too much with significant vision and balance disturbances, dizziness, warm sensation sweating, it doesn't have the brain fog of alcohol even at high doses. Duration is short, no more than 4-5hrs to baseline.
Onset is 30mins and it builds do not try and titrate doses based on initial effects. it is similar in some ways but different to alcohol. It synergizes with alcohol but not necessarily in a good way.

The individual enantiomers have been tasted, the S enantiomer is much more than 2x more potent, as a sedative and is much more physical than the racemate it also does not have a linear dose response 50mg of S is approaching 160mg equiv of racemate. R is somewhat elusive effects-wise, it clearly does something but it is easy to ignore it is more of a mood improver and subtle, highest level of R was 50mg.

How either enantiomer actually works is not clear, or whether one enantiomer antagonizes the other.

Merck and GSK have a bunch of unpublished information on this compound as do Pfizer who developed modifications in the 1990's

 

[negrogesic]

^^^^this is very much appreciated and very helpful

I think i felt something with 12mg, but it was combined with over a bottle of wine. With my eyes closed i noticed a brightness that i often see with alcohol and gbl.

 

[negrogesic]

HA-966 second trial: 36mg

Was in a terribly depressed mood, quite anxious (some of it stemming from mild tianeptine withdrawal. First attempt at 12mg was only slightly perceptible.

I was surprised to begin feeling it after only 10 minutes. First manifested with a rapid antidepressant effect, slight tiredness. Mood is significantly improved. Antidepressant effects continue to grow, after about 30 minutes some sedation and paradoxical stimulantion (perhaps the GHB receptor is involved?). Sedative properties grow, as do anxiolytic properties, and seem to peak after 40 minutes. It has been 63 minutes at the time of writing and i cant see the effect increasing from here. Reminds me of a cross between 1,4-butanediol, ethanol and dextromethorphan. There is some nausea and dizziness, and i could imagine a large dose being potentially quite nauseating. The dizziness seems disproportionate to the inebriated.

I doubt high doses would be euphoric like GHB or its various prodrugs but the relief of anxiety and depression is quite therapeutic and in that regard you might say it could have the sort of recreational that benzos can have. Not as clear headed as I hoped (I feel a bit distracted), and a little inebriated. This limits its therapeutic potential as it would impair driving and overall functioning more so than an equianxiolytic dose of benzodiazepines. This has an antidepressant effect that benzos clearly lack however. 36mg was surprisingly strong, I was originally going to go with 50mg, but im glad I didnt as I don't want to be that incapacitated at the moment. I could see it as a usual alternative to benzodiazepines for acute anxiety with depression. I almost felt like reaching for a benzo this afternoon due to anxiety, and now i have no intention to use one (which is good, because due to past severe benzo dependencies, a single good dose will cause rebound anxiety for days).

 

[sekio]

I wonder how it combies with marijuana?

 

[negrogesic]

I had a little marijuana after 60 minutes but not enough to be able to characterize the combination. Its unclear how well they'd work together since i havent combined 1,4-butanediol (which is the single closest substance this reminds me off -- though its not a fair characterization, just the closest) with large amounts or marijuana. Might increase the dizziness and disorientation. Alcohol, phenibut and benzos would seem like better partners, could be wrong. Never combined GHB and marijuana, which would also give you an idea of the combination potential.

Its been about 3.25 hours now since the 36mg dose and though i think it is mostly worn off, perhaps some antidepressant properties remain, its hard to say as ive since had 2 beers. What was most striking was the fast acting antidepressant properties. Definitely useful stuff, I'll carry some 30mg doses in my wallet to have as a fast acting anxiolytic/antidepressant for severe anxiety or intractable bad moods that could benefit from pharmacological intervention. Ive noticed 1,4-bd and gbl share this foul mood reversal properties, but have even more nausea and more side-effects (and are hard to store in ones wallet).

 

[negrogesic]

As an update I had an additional 25mg at t+6 hours, then another 60mg at t+8.5. Did help induce sleep but the NMDA-antagonist properties are pretty clearly perceptible at 60mg, which can at the same time make it harder to sleep. As i was laying in bed there were some sinister closed eyed visuals reminiscent of those i get from some dissociatives (particularly nitrous oxide), which consists of colorless metalic-gray forms depicting somewhat violent sexual imagery. Its not the most pleasant thing in the world when you are trying to fall asleep and is clearly characteristic of NMDA-antagonist activity for me. This was eventually followed by sedation. The psychotomimetic properties thus limit its usefulness as a sleep aid for me (as does its 5 hour duration of action), but it holds good promise as an occasional daytime rescue antidepressant or anxiolytic.

 

[negrogesic]

Update: i find this stuff shines at 20-23mg as a daytime subtle (yet not so subtle) anxiolytic and antidepressant. Only mildly sedating and doesnt significantly impair cognition, though a slight disconnection/spacey feeling is certainly there.

 

[llamer]

Yeah NEGOGESIC has it right, those are the feelings I'd associate with the dosages. A higher dose around 100 mg will bring on a unique tired form of feeling, it sort of depends on how sleepy you really are. But the sleep is good, i never noticed a GHB like 5 hr rebound, the whole thing is far more subtle (perhaps with those isolated racemates one could discern). If the price goes down I'd like to keep some around. I'd like to know how it interacts with adaptagenic herbs like ashwagandha and gotu kola

 

[dopamimetic]

Oh fuck now I just posted about the strange effect of snorted memantine and now this. Exact the kind of drug I am currently looking for as next research material.- Got on my list. Maybe I'll dream about your purchase some night and the dream leading to the vendor? xD

(OT: Why isn't there an advanced discussion board where sourcing and sharing is allowed .... guess in times of TOR and I2P technology won't be the problem ... and if done correctly, that should neither attract police (no deaths, no reckless intoxicated teens) nor whatever else. Ok, I get it, such a thing will exist, more than one, but without real life contacts there is no entrance for me. WTF it's not my fault that I didn't have equal start chances in life and now have to fight for everything by myself and against the state I indeed would like to stay behind but can't as it declares me illegal by trying to help myself and to do science.

As I don't believe to be something extraordinarely special, I guess there must be some more of my kind. It's just the fools mob ruining everything remotely accessible from the outside..

 

[higherconciousness]

Well I tried approximately 150mg over the last hour and a half and don’t feel much. Not sure if it’s the other drugs I’m on. I took a small dose of memantine and a gram of NAC which is notorious for reducing the effects of a wide range of drugs.

 

[higherconciousness]

I dunno. I just took an unknown amount of bromazolam. I spilled my solution of bromazolam the other day. There may have been 20 mg or so left so I took some cotton swabs and soaked as much up as I could. I took the biggest Swab, I can’t imagine it’s being more than 5-8mg at the most. Let’s see what happens now.