[FollowingTheDao]

Tofisopam is a type of benzodiazepine, yes? Benzodiazepines are depressants that enhance the effect of the GABA, and the literature suggests that tofisopam does not act on the GABA-A receptor but it does enhance the binding of other benzodiazepines to their binding sites.

Any increase in GABA will counteract the excitatory transmission of Glutamate. That is all that matters.

But I know klonopin can eliminate my Tinnitus. So if you can explain how that works go right ahead.

[The_rationalist]

> Any increase in GABA will counteract the excitatory transmission of Glutamate. That is all that matters. No that is not all that matters. The main effect of tofizopam is unrelated to GABAergy, the fact it indirectly modulate GABA-A and potentiate benzos is a plus but its main effect come from atypical PDE inhibition. Look if klonopin is viable for you and solve your tinnitus that's great to hear. But for many people regular benzos are not a complete solution. Tinnitus is a multi-factorial condition and some people might get better results that other with a given medication.

> if you can explain how that works go right ahead Tinnitus is an excitatory overload localized in audition related neuron circuits. AKA too much glutamate (mGLURs, AMPA, NMDA, kainate). The brain is mostly a mixture of excitation (GLUT) and inhibition (GABA-A, B). By taking a classical benzo like klonopin you increase your GABA-A level which inhibit the overload of excitation (GLUT). That is why it works. You can also lower you glutamate levels independently of you GABA via an NMDA antagonist such as memantine. Those two mechanisms are the basic treatments to tinnitus. However there are more specific mechanisms (PDE, synaptotophics, calcium blockers, anti oxidants, bioenergetics) that can be complementary. Classical benzos and NMDA antagonists are not enough for some people with tinnitus.

[FollowingTheDao]

> The main effect of tofizopam is unrelated to GABAergy

It's a antagonist of the AMPA receptor. I am not saying it has anything to do with GABA-A but it enhances the action of GABA.

https://www.nature.com/articles/nn0600_551

>By taking a classical benzo like klonopin you increase your GABA-A level which inhibit the overload of excitation (GLUT).

No, Klonopin does not increase GABA, it attaches to the GABA-A receptor to allow more chloride into the cell. It only enhances the activity go GABA.

https://en.wikipedia.org/wiki/Clonazepam#Pharmacology

[The_rationalist]

I have not found information saying that tofisopam is an AMPA antagonist. But you are probably right, the answer must be on the paper you link I guess. Nevertheless the action on PDEs is what makes tofisopam unique.

> No, Klonopin does not increase GABA Yeah that's right. GABA releasing agent, GABA reuptake inhibitor and GABA transaminase inhibitors do exists but benzos have not those properties. They are GABA-A positive allosteric modulators (they are not agonists although GABA agonists do exist too). So yeah they potentiate GABA functionally without increasing its quantity directly.