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HA-966

negrogesic

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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

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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

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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

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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.


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

polymath

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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

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Screenshot_20200116-125516_Chrome.jpg

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?
 
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