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GABA, its derivatives (Phenibut specifically) and its effects on the brain

gaba phenibut temporal lobe tolerance agonist auditory memory long-term

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6 replies to this topic

#1 sparkk51

  • Location:TX, US

Posted 07 June 2012 - 12:40 AM


Hi,

recently I purchased Phenibut as I had assumed at the time that it would be the most appropriate GABA supporting drug. However, various posts in this forum, as well as in others, indicate that it is extremely impractical to use on a long-term basis considering tolerance. This surprised me as I thought Phenibut would be the perfect GABA-receptor agonist due to the fact that it is basically GABA but with the ability to cross the blood-brain barrier. Here are some questions I have for Phenibut and other GABA agonists:

Considering Phenibut is, as I said earlier, a very simple derivative of GABA itself, wouldnt that imply that the noted tolerance it produces be an effect of down-regulation of GABA receptors instead of some other mechanism which inhibits (specifically) Phenibut's mode of action? May we assume that finding a proper long-term GABA agonist is futile?

Does the tolerance that arises from using Phenibut only occur when more than a certain dose is taken per day?

I have this intuitive sense that all the ill-remarks directed at phenibut are really, deservedly, for the GABA system itself. Otherwise, wouldn't it be implied that there is some substance out there which effectively agonizes GABA receptors while not producing tolerance for an appropriate amount of time?


Now, as for the effects of the neurotransmitter itself; does GABA have a strong connection with temporal lobe functions? I believe I read somewhere that GABA is produced in this area of the brain, although I wouldnt be surprised if I was mistaken. The reason I ask is because I believe I have weak temporal lobes considering my poor recollective memory and auditory processing.

Perhaps, if it is appropriate, ill be able to share a MRI of my brain and receive input on what component of my brain seems weakest... That sounds really silly but what the hell, this is the internet.

Thanks!
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#2 jadamgo Re: GABA, its derivatives (Phenibut specifically) and its effects on the brain

  • Location:USA

Posted 07 June 2012 - 07:06 PM

Considering Phenibut is, as I said earlier, a very simple derivative of GABA itself, wouldnt that imply that the noted tolerance it produces be an effect of down-regulation of GABA receptors instead of some other mechanism which inhibits (specifically) Phenibut's mode of action? May we assume that finding a proper long-term GABA agonist is futile?

Does the tolerance that arises from using Phenibut only occur when more than a certain dose is taken per day?

I have this intuitive sense that all the ill-remarks directed at phenibut are really, deservedly, for the GABA system itself. Otherwise, wouldn't it be implied that there is some substance out there which effectively agonizes GABA receptors while not producing tolerance for an appropriate amount of time?


Now, as for the effects of the neurotransmitter itself; does GABA have a strong connection with temporal lobe functions? I believe I read somewhere that GABA is produced in this area of the brain, although I wouldnt be surprised if I was mistaken. The reason I ask is because I believe I have weak temporal lobes considering my poor recollective memory and auditory processing.


Whether it's futile to find a long-term GABA agonist or not depends on what you want to do with it. Phenibut and baclofen can be effective long-term anti-spasticity agents for use in spinal injuries, multiple sclerosis, cerebral palsy... But long term anxiolytic effects are harder to sustain.

It's not impossible to use it for long-term anxiety relief, but some people can do it and others can't. It depends on what type of anxiety you have, and what the triggers are, and how well you're using coping skills... that sort of thing.

What is clearly not sustainable is using phenibut (or baclofen) as a sleeping aid. That does not work. In fact, no GABA agonist sleeping pill works well over the long term. They give you amnesia so you forget lying in bed awake, then you assume you got good sleep. But you didn't get better sleep -- all current sleeping pills only add 5-20 minutes of sleep to your nights in the short term. Over the long term, some of them continue to give you an extra 5-10 minutes, but some of them quit working entirely. That's why I always recommend CBT-I over sleeping pills; it's the only truly effective option. Sure, it's harder to modify your behavior than to pop a relaxation-and-forgetfulness pill every night, but CBT-I cures the insomnia and the pill doesn't. That's the only thing that really matters if you suffer from insomnia.

Anyway, back to GABA agonists. The GABA system is pretty plastic, so yeah, tolerance does develop to any GABA-A or -B agonist if you're using it daily. Simple fact. But when using a benzo (or phenibut) responsibly, the tolerance often stops at some point where you're still getting effective help for anxiety. As long as you DO NOT escalate the dose further (chasing euphoria or sleep), you can probably stay on that same dose for years at a time. I know plenty of people on long term treatment with daily clonazepam, and it works fine. In the past, I've used MRM Relax-All with Phenibut safely. It contains a very low dose of phenibut -- I believe it's 500mg per 4 capsules. I'd take 1-2 capsules before social events that caused anxiety, and the anxiety would be significantly reduced. I only did this about 6-10 days out of the month, and I never had a problem with tolerance or withdrawal.

People who use phenibut to get high DO have tolerance and withdrawal. They escalate their dose, sometimes taking tens of grams per day. Not milligrams, but grams. That's very unhealthy. But using phenibut as I described, a few hundred milligrams 1-3 times a week, is perfectly safe. In fact, I'd still be using phenibut before social events if I hadn't cured my anxiety with psychotherapy.
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#3 sparkk51 Re: GABA, its derivatives (Phenibut specifically) and its effects on the brain

  • Location:TX, US

Posted 07 June 2012 - 09:43 PM

Thanks for the response jadamgo.

Would you know anything about a synergy of sorts between GABA and L-Glutamine supplementation? I recall last week I took a fraction of a teaspoon of L-Glutamine and had extraordinary cognitive results for the rest of the day. Alas, the next few days I had received no benefit from it whatsoever. Yesterday, I had taken phenibut and a deep prolonged sleep of approximately 12 hours followed. I took L-Glutamine again this morning, as usual, and am feeling the same results as the first day I had taken it. I do know that Glutamate is the precursor to GABA. I do not know whether I should contribute the cognitive improvement to good sleep, L-Glutamine supplementation, or both.

Also, are you suggesting that daily intake of phenibut is impractical?

Edited by sparkk51, 07 June 2012 - 09:45 PM.

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#4 sparkk51 Re: GABA, its derivatives (Phenibut specifically) and its effects on the brain

  • Location:TX, US

Posted 09 June 2012 - 06:06 PM

Do you think that after taking Phenibut, taking a supplement which increases Glutamate could lessen tolerance? I question this considering GABA is needed to moderate Glutamate transmission, correct?
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#5 medievil Re: GABA, its derivatives (Phenibut specifically) and its effects on the brain

  • Location:Belguim

Posted 15 June 2012 - 07:30 AM

I took 8 gram a day for some time it worked quite a long time didnt notice much tolerance however for many its a big issue with it. If you have little tolerance and can block and are prepared for the withdrawal in case that may happen (physical dependency occurs fast but taking some valium for a week and you wont feel it) then it could be used daily.

Question is how, i think some said nmda antagonists blocked tolerance but there arent enough anecdotes to come to conclusions.
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#6 Nootr Re: GABA, its derivatives (Phenibut specifically) and its effects on the brain

  • Location:Spain

Posted 28 June 2012 - 10:07 AM

The maximum i have taken was 0.75 gram per day. That is three tablets of 0.25 g. That is quite enough to get rid of acute anxiety. The world around you becomes "dreamy" and you percieve it as a dream.
The effect of phenibut depends on the manufacturer. I have found only one good phenibut amoung 4 which inreases mood sufficiently good and which acts like a "pill of truth" with seeing the things around in bright-light aura. I don't know to which degree manufacturers are honest since onle one company among 4 is doing good phenibut. There is also a probability that this "good" company addes some other substances to phenibut which makes it so good but does not declare it to public.
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#7 golden1 Re: GABA, its derivatives (Phenibut specifically) and its effects on the brain

  • Location:US

Posted 28 June 2012 - 05:04 PM

I think if you want to use phenibut as a nootropic, you have to dose very low... like 50-300mg/day and take weekends off or something. if youre looking for something to support gaba, maybe l-glutamine + b6/p-5-p + riboflavin + thiamine(used to make gaba). Most things that are agonists arent really going to work long term, many nootropics happen to not really have a direct agonist action, instead working on ion channels, ampa/nmda/glutamate modulation, and whatever else. This applies even more so to gaba receptors(alcohol/benzo/etc withdrawal) and certainly 5ht2a receptors(psychedelic tolerance)
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Also tagged with one or more of these keywords: gaba, phenibut, temporal lobe, tolerance, agonist, auditory, memory, long-term

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