• N&PD Moderators: Skorpio

GABA Receptor Antagonists

This thread is like someone saying they got chemical burns from potassium hydroxide years ago and that they're now trying to remove the scars with conc. sulfuric acid...
No, it actually works (for alcohol or benzodiazepine tolerance) according to a paper i found a few weeks ago with Pentylenetetrazol (if i remember correctly) in mice.
Im sorry i don't have the reference right now, but i don't think it's a new or too interesting idea... 8)

BTW: I don't think it has any practical use in human subjects, because of way too many side effects.
 
what, you don't think we should start administering pentylenetetrazol to humans? Bah! Convulsive therapy for all!
 
Cool, looks like I'm stuck with benzos forever. Was RX'd 16mg of clonazepam for ~4.5 years, taken off it, and developed epilepsy. I'm in the process of weaning of Keppra right now, as the last 2 years on it have been worse than having a seizure every now and then. Good times.
 
How exactly is repair possible?

Surely it can't be as simple as flicking a switch for example?
I guess it'd be a week to month long painful process of convulsive therapy with Pentylenetetrazol.
It doesn't have to be painful but at least long and completely experimental with widely unknown side effect but likely much anxiety...

PS: Without proper medication very much like torture.
 
It is? It was an approved drug for decades. It's known to enhance memory formation (Psychopharmacology, Vol 12, No 4 (1968), 303-321, DOI: 10.1007/BF00401409), is probably beneficial in down syndrome (Neurology Today, Vol 7 Iss 7 pg1-17 doi: 10.1097/01.NT.0000269122.67974.02). If it's neurotoxic it's apparently in a very minor way. Unlike commonly used anticonvulsants like valproic acid and benzodiazepines which is well established.

just to be clear, though, I wouldn't really advise it either. Flumazenil might be safe enough to do for a non dependent person. PTZ not a great idea.

I was trying to goooggggleeee a bit to see if there were any agonist derivatives of PTZ. It would be interesting to know if adding a benzo ring on there and an appropriately located phenyl group might yield an agonist. I dunno why- they don't even bind to the same site.
 
i believe chronic alcohol abuse causes oxidive stress causing neurodegeneration...

you'd need to find a drug which doesn't antagonize GABA receptors but rather promotes regeneration of neurons in the brain... good luck with that one8(

nf-kb binding is also another problem with alcohol as it's incorrectly regulated when alcohol is present in the system, with chronic use it becomes a more serious matter... i'm not sure if that can be reversed, but possibly inhibited while alcohol is used?

http://onlinelibrary.wiley.com/doi/10.1111/j.1530-0277.2000.tb01973.x/abstract

this looks interesting regarding damage, but nothing to answer your question... i don't have access to this - but from the abstracts it seems as if you'd have to repair the limbic system of the brain. ouch.
 
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