Anyone heard of glyx-13? I think its a true wonder drug...

Yes sir, I have been looking into a supplier to get my hands on some. The prices I am finding are ridiculous though.

GLYX-13 is a very interesting compound. People are commenting that it is like ketamine, but that is incorrect.

I made this figure the other day when I commented on another thread speaking about GLYX-13.

As you can see, it has a very unique binding compared to other NMDA modulators. Ketamine is a non-competitive antagonist that binds at an allosteric binding site on the NMDAR. It completely blocks the ion channel from opening, regardless of membrane voltage potential, magnesium blockage, or glutamate/glycine binding. Ketamine also blocks the channel itself in a similar fashion to magnesium, but it's not voltage-dependent. This basically means that it's an off switch. This is where the dissociative properties arise from.

Magnesium itself is a voltage-dependent channel blocker. This means that it will block the ion channel even if glutamate and glycine are bound to the NMDAR. However, if the neurons membrane voltage rises above -40mV, then the magnesium unbinds and allows the ion channel to open. This is good, because it protects the neuron from glutamate excitotoxicity, but still allows for normal operation once the neuron becomes excited.

Memantine is another NMDAR antagonist. However, it has a totally different binding site than the others. It's site lies within the channel itself. This means that it cannot bind unless the neuron reaches excitability, magnesium ceases blocking the channel, and the channel opens. This makes memantine a much better drug than ketamine, because it's an intelligent off switch, not just a total one.

Now on to GLYX-13. This one is really cool for a couple different reasons. One, it binds to the glycine site, which is a new class of NMDAR modulators. Two, it is an agonist/antagonist. This means that it can activate the NMDAR and deactivate it depending on the electrical conditions. The racetams also work in this manner, but at an allosteric site. Aniracetam in particular has very similar effects to GLYX-13, just at the allosteric site instead of the glycine site. The advantages of this are enormous. Not only can it protect the neuron from too much calcium influx, it can increase the efficiency of the calcium influx as well.

I am VERY interested in this substance, especially given the human trials that have been done. It's actions are a much more intelligent way of modulating the NMDARs, rather than total blockage from ketamine or other similar substances.