Affect of benzodiazepines on GABAa receptors

[.:Holy::Toast:.]

So as its my understanding benzodiazepines exert their action mainly via a positive allosteric modulation of the GABAa receptor type, now does this increase the efficacy of the endogenous ligand when it binds or does it only increase the constitutive activity at these receptors in general, regardless of whether there is an agonist oresent.

Essentially what im asking is if could one suplement with GABA for a week or so before hand and experience potetiated effects from benzodiazepines or does the increase in GABAa efficacy arise solely from the conformation change induced by the allosteric modulation by benzos

 

[sekio]

BZDs increase the effect of GABA at receptors e.g. it needs an agonist present for them to produce an effect.

Supplementation with oral GABA or glutamate doesn't do anything for GABA levels in the brain though (otherwise it would be Rx for anxiety and also be intoxicating at a certain dose... neither of which are the case)

 

[Solipsis]

It is intoxicating indeed I would say, but the effect is very transient. Too transient to be useful. I get a lot of flushing followed by sedation / relaxation. Of course I could never rule out placebo on my own, but fwiw it was a marked effect.

What about drugs that influence GAD though?