Comment · Mon, April 29, 2013 · Ceretropic
"I continue to discourage personal use until the drug is proved to be safe." - Fulvio Gualtieri, former researcher on sunifiram.
Original post in this thread
shrillthrill · 62 points
Just a reminder that not everything labelled nootropic has been demonstrated safe in humans, despite it being available to buy from NSN.
What they were answering
AtomikPi · 6 points
I would just like to add that the dosages used in rats are extremely low. If you scale them to human doses allometrically, they are under 1 mg. If you compute the equivalent of the 1000x doses in humans, they work out to around 200mg or so. So the ratio is more like 20x.
And regardless of whether it's an NMDA modulator, it's my understanding that it's an AMPA modulator as well. That means there's potential for excitotoxicity. It's unlikely, perhaps, but it's possible.
u/MisterYouAreSoDumb · Ceretropic
Given the study I linked, the AMPA theory seems to be less likely.
In this study, treatment of gavestinel, a glycine-binding site of NMDAR antagonist prevented the enhancement of memory-related behaviors by sunifiram in Y-maze task or novel object recognition task.
>We also observed that enhancement of LTP by sunifiram concomitant with increased CaMKII autophosphorylation in OBX
mouse hippocampus is totally blocked by gavestinel treatment,
suggesting that sunifiram preferentially activates CaMKII post-synaptically via stimulation of glycine-binding site of NMDAR. The elimination of PKC autophosphorylation and NMDAR phosphorylation by gavestinel treatment also suggests
that glycine-binding site stimulation by sunifiram is critical for enhancement of NMDAR function and LTP through PKC.
It does affect the transmission of calcium into neuron, though. So it has the potential, in theory, to cause excitotoxicity. Not that I am saying we should not proceed with caution. I agree we need more information on this substance. However, everything I see so far points to it being safe. That doesn't mean that we will not discover something down the road that changes that stance.
Also, keep in mind the doses were intraperitoneal. That means they may not transfer directly to sublingual, even after taking allomteric scaling into consideration.