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Lets talk about GABA (as a supplement) again

Jamshyd

Jamshyd

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Ok, I was scanning the forums for opinions and studies, and this seems to be about as inconclusive as the Loperamide question.

So lets open this can of worms again. What say ye, o wise ones?

I never tried this due to the prominent idea that GABA is innefective due to not crossing the BBB. Then I find people claiming that it can do that via active transport. In any case, I'll probably pick a bottle of this (since its cheap) tomorrow and give my input. Till then, let me know what you think.
 
I remember reading on BL somewhere that it does have the ability to cross the BBB, just not very well. By using huge amounts of GABA, some people reported some relaxtion and whatever...but also numbness in the extremities 8o
 
Well, I recently purchased 10 grams and had 4 seperate doses of it- and every time I got very very strange 'symptoms'. A feeling of extreme salvia-like parathesia, mainly aroung my upper body and chest, brief euphoria, increased anxiety (mainly because I was completely unaware that GABA would have any perceptible effect)....The feeling was not that of a supplement, but a real drug. I know thats a useless kind of statement; but I was really taken aback by the feeling. I have no idea what the dosage is meant to be, so perhaps I overdid it.
 
^ I personally found L-Theanine much more useful with less negative effects, but to each their own.

In any case though, this thread is about just GABA, so lets keep it there please :)
 
swilow said:
Well, I recently purchased 10 grams and had 4 seperate doses of it- and every time I got very very strange 'symptoms'. A feeling of extreme salvia-like parathesia, mainly aroung my upper body and chest, brief euphoria, increased anxiety (mainly because I was completely unaware that GABA would have any perceptible effect)....The feeling was not that of a supplement, but a real drug. I know thats a useless kind of statement; but I was really taken aback by the feeling. I have no idea what the dosage is meant to be, so perhaps I overdid it.
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2 grams is normal but you can(and sometimes have to) take more then that, it's pretty harmless. If you noticed a real effect from it then you probably are low in it which more then lickely translates to having problems with anxiety and sleeping.
 
That whole not crossing the blood brain barrier issue is really not clear to me. I have yet to read any studies that make conclusive claims that it is not able to cross the bbb at all. If anyone has a link or something I'd appreciate it.
As far as personal experience goes, I have felt that taking GABA during benzodiazepine withdrawals really helps with withdrawal symptoms and it's not placebo. Sadly because of tolerance I've had several cold turkey benzo withdrawals to date and the ones when I didn't take GABA supplement, pure GABA tablets actually not GABA+ something else, were much worse. It also seems to augment the benzo high to an extent.
 
GABA at doses around 1-2 grams gives me an anxious feeling of shortness of breath. It truly sucks. And yeah, I get the tingles, too. Not worth the trouble. Phenibut, on the other hand, is totally nice, until you try to stop :)
 
^Assumedly, heaps. GABA receptors are amongst the most abundant. I'm inclined to think its effects are almost solely from peripheral-stimulation/inhibition.

2 grams is normal but you can(and sometimes have to) take more then that, it's pretty harmless. If you noticed a real effect from it then you probably are low in it which more then lickely translates to having problems with anxiety and sleeping.
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I have little trouble sleeping, though I only sleep for four or so hours a night...but yeah, am plagued by anxiety.
 
^^^
feels like the peripheral effects of good kava to me... works for most anxiety in doses as low as 100-200mg daily, especially those that seem to be related to bloodsugar eg. ex-tweakers and potheads...

small amount may cross the BBB but the major action is mediated at GABA-b sites by GAD (glutamic acid decarboxylase)

GABA_synthesis.gif
 
there is no evidence that GABA can cross the BBB, in fact all the evidence not produced by supplement manufacturers points to it not being able to cross.
so if it works then it would seem tome to either be peripheral or acting by some other indirect pathway.

Because of the importance of GABA as an inhibitory neurotransmitter, and its effect on convulsive states and other motor dysfunctions, a variety of approaches have been taken to increase the brain GABA concentration. For example, the most obvious approach was to administer GABA. When GABA is injected into the brain of a convulsing animal, the convulsions cease (Purpura D P, et al, Neurochem. 1959;3:238-268). However, if GABA is administered systematically, there is no anticonvulsant effect because GABA, under normal circumstances, cannot cross the blood brain barrier (Meldrum B S, et al, Epilepsy; Harris P, Mawdsley C, eds., Churchill Livingston: Edinburg 1974:55. In view of this limitation, there are three alternative approaches that can be taken to raise GABA levels.

The most frequent approach is to design a compound that crosses the blood brain barrier and then inactivates GABA aminotransferase. The effect is to block the degradation of GABA and thereby increase its concentration. Numerous mechanism-based inactivators of GABA aminotransferase are known (Silverman R B, Mechanism-Based Enzyme Inactivation: Chemistry and Enzymology, Vol. I and Il, CRC: Boca Raton 1988).
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however the 2-pyrrolidinone which is to gaba what gbl is is to GHB might be able to cross, and there are plenty of other GABA prodrugs that can. somewhere there must be a radiolabelled distribution study on GABA, but I haven't got time to find it.

Biomed Mass Spectrom. 1979 Jan ;6 (1):23-6 427258
Detection of the in vivo conversion of 2-pyrrolidinone to gamma-aminobutyric acid in mouse brain.
[My paper] P S Callery , M Stogniew , L A Geelhaar
Labeled gamma-aminobutyric acid was detected in mouse brain following intravenous injections of deuterium labeled 2-pyrrolidinone. [2H6]Pyrrolidinone was prepared by the reduction of [2H4]succinimide with lithium aluminum deuteride. Quantification was accomplished by a gas chromatography mass spectrometry assay method. gamma-Aminobutyric acid and internal standard, 5-aminovaleric acid, were converted to volatile derivatives by treatment with N,N-dimethylformamide dimethyl acetal. Quantitative estimates were derived from peak area measurements obtained from monitoring the parent ions of the gamma-aminobutyric acid and internal standard derivatives by repetitive scanning during the GC run. The conversion of pyrrolidinone to gamma-aminobutyric acid may provide a method for labeling central gamma-aminobutyric acid pools.
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there is a whole world of real info beyond the Wiki.........
 
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^that sounds interesting, i wonder if the 2-pyrolidinone has the same effects on humans?
 
Many esterfied analogues of GABA probably have anxiolytic activity/abuse potential:

Ester derivatives of gamma-aminobutyric acid (GABA) and GABA analogues which cross the blood-brain barrier are disclosed, as well as methods of synthesizing and using the compounds.
...
Additionally, since the attachment of these compounds to GABA and GABA analogues is through an ester bond, these derivatives act as prodrugs which may be hydrolyzed in situ providing a means to increase GABA and GABA analogue levels in the CNS. Given the different characteristics of the groups attached to GABA and GABA analogues, the rate of hydrolysis will be different for different GABA and GABA analogue ester derivatives. Thus, shorter and longer acting compounds, having GABAergic activities, are produced.
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http://www.freepatentsonline.com/5051448.html

Easy synths
 
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^ So if I understand correctly, this quote confirms that the esterification of GABA into more BBB-friendly things can happen inside the stomach if all the proper ingredients are present?

I ask because I've seen GABA marketted with B6 with the claim that it converts in the body to picamilon.
 
How? Carboxylic acids aren't all that reactive and I doubt that the niacin would be converted to an acyl chloride in vivo.

The esters are so easy to prepare you may as well make them, anyone with a high school science lab could probably prepare a number of them.
 
this is somewhat unrelated but i found that initially gaba helped me tremendously in falling asleep, but as i took it more and more i developed a semi-permanent tolerance, and the dosage has skyrocketed from 500 mg to 3 grams and still not doing what it used to, i guess this happens with most substances out there
 
Jamshyd said:
^ So if I understand correctly, this quote confirms that the esterification of GABA into more BBB-friendly things can happen inside the stomach if all the proper ingredients are present?

I ask because I've seen GABA marketted with B6 with the claim that it converts in the body to picamilon.
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This sounds unlikely, you got any articles to confirm? That reaction really seems like bogus to me. 8(
 
uacvax said:
this is somewhat unrelated but i found that initially gaba helped me tremendously in falling asleep, but as i took it more and more i developed a semi-permanent tolerance, and the dosage has skyrocketed from 500 mg to 3 grams and still not doing what it used to, i guess this happens with most substances out there
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Amino acids are only meant to be taken over a short period of time , then you will need a break. Month on month off for most, 5-htp can be taken 2 months on one month off.
 
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