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N&PD Moderators: Skorpio
Do GABA antagonists upregulate GABA receptors?
- Thread starter seep
- Start date
love2party
Bluelighter
Gaba antagonists would probably be horrible to be on, you brain would be too overstimulated.I'm not sure about an antagonist at the GABA binding site but the benzodiazapine antagonist flumazenil has been successful in treat paw symptoms. Considering it's ability to treat ongoing withdrawal symptoms, I would say that would indicate the benzodiazapine site was returning to normal as a result of its antagonism. It would be an awful idea while dependent on benzodiazapines though.rollingstoned!
Bluelighter
I'd be suprised if they didn't. I'd imagine they'd suck to be on, but coming off would be greaat.hamhurricane
Bluelighter
...Indian on flumazenil said:^that is an awesome quote. I love it.
for various drugs, yes. It is believed to, oh shit...
I see now that it's believed to selectively antagonize upregulation of GABAA receptors containing alpha-4 subunits. I guess it deactivates transcription.
That's the opposite of what I expected. I see no data on it enhancing upregulation.
Nevertheless, flumazenil obviously isn't the only BDZ antagonist around. We even have endogenous antagonists (like DBI).
There's a chance some here have taken GABA antagonists without knowing. If you've ever had proper absinthe, or certain types of martini, or chicken vermouth, or anything with wormwood in it (like wormwood).You're right, an increase in functionality isn't always associated with an increase in receptor density. I think flumazenil just helps fix the fucked up gaba a receptors after extended benzodiazapine use.
http://onlinelibrary.wiley.com/doi/10.1111/j.1471-4159.1988.tb04848.x/abstract
An antagonist at the GABA binding site is probably more likely to result in an increase in receptor density. This study shows an increase in GABA a receptors.