View Full Version : GABA - Blood Brain Barrier

14-11-2004, 03:56
Is taking supplements of GABA in its pure form (gammo amino butyric acid = GABA by the way - i'm sure you all knew that, anyways, i'm rambling, back to topic).

I have heard that GABA itself does not cross the blood brain barrier very well at all, and therefore taking GABA supplements is futile, at least for any kind of recreational purposes.

Anyone know? Also, would taking GABA supplements in high dosages increase the recreational value of drugs that specifically react upon GABA? (i.e. benzodiazepines, GHB, hmmm, maybe even alcohol) ?????

14-11-2004, 10:07
It's highly unlikely that GABA gets good access to the brain, but, from my reading of the literature, high doses of GHB (5-15g) do cause an effect in the human brain... They both get into the blood, and get into the brain...

Is it caused by GABA itself? I don't know, for all I know, it could get caused by GABA turning into GHB... Because I don't know the mechanism, I can't comment on what effects it would have on other drugs, but I would be very careful about mixing it with other depressants.

15-11-2004, 08:35
Got any links or references of "your reading of the literature"?

15-11-2004, 10:53
Yeah, but "GABA" into pubmed.
But more specifically, this (http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=15469644) and this (http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=pubmed&dopt=Abstract&list_uids=7376786).

There is a variety of them out there, though I find them fucking hard to find when I want them.

15-11-2004, 11:29
Just some anecdotal information. I have used gaba as a supplement, and it did effect me mentally ( relaxed, slightly drowsy). It does not seem to have any recreational effect. It did effect phenobarbital's effect on sleep. If i would take it a day after taking phenobarbital my sleep time would increase compared to a non-gaba night after phenobarbital.
I have read what you mention too. Gaba is not suppposed to cross the blood-brain b. , so why does it have an effect? I think the transport to the brain might just not be that efficient. If three grams of the ingested gaba would all go to the brain one would probably not be able to keep awake!

15-11-2004, 23:53
That's basically what I think smartshop... GABA probably has very poor brain access.. but if you eat 15g of the shit, and only 0.001% got to the brain, you would still get an effect. Though there's also the possibility it has some downstream effect, getting gonverted into some amino acid, or blocking somethings transport into the brain, or something.

16-11-2004, 06:43
I've been taking 1200 mg of it in combo with klonopin, and have noticed a diffference in the euphoric effects of the kpin every time. Also, ive been taking kpins for months, so I am not biased by any placebo - in fact, i actually took the GABA supplement the first time in combo with the kpin thinking it was a different one (tyrosine). Its recreational benefits though, at least with kpins and in my limited experience are not anything to jump and dance about. Still, why not? GABA definitely couldn't HURT or DECREASE the recreational benefits of any GABA releasing drug (benzos, alcohol GHB etc.)

16-11-2004, 08:10
I love how people on this board think they are immune to placebo effects... Unless you had no idea that you were getting a drug, you can't be rule out placebo effects.

30-05-2011, 07:56
I had been taking Gaba, among other things for anxiety but to little effect. I just learned that theanine, about 200mg, releases GABA into the brain. It may be too soon to tell but I swear my anxiety level has gone way down. I am beginning to believe that GABA itself does not cross the blood/brain barrier and that theanine is far superior to boost GABA levels. Does anyone have any useful info on this subject?

30-05-2011, 14:54
GABA does not cross the BBB i don't think. I believe it is too hydrophilic.

31-05-2011, 18:59
It's highly unlikely that GABA gets good access to the brain, but, from my reading of the literature, high doses of GHB (5-15g) do cause an effect in the human brain... wth is blizor talking about of course GHB, high doses has an effect?

yah gaba somehow converts to ghb
some ppl say that gaba can be an antidepressant, I find it is that way. through eating it(especially gaba rich food I find this) and getting a restfull sleep.

28-05-2012, 02:21
At 5grams I get a transient (a few minutes) shortness of breath and parastethis (tingles)...not that uncomfortable, but it lets you know its "hitting". It knocks me out and after using it for over a week it lasted during the day for me having an anxiolytic effect.

I've had insomnia all my life and hated the sides of ambien and the ilk. Melatonin, Valerian, etc. gve me little reprieve and when I started doing GABA it was miraculous.

I'd love to hear an explanation, because I've had ten other people I've recommended it to take 3-5 grams at night and ALL saw deeper sleep and more dreaming.

30-05-2012, 19:04
Gamma-aminobutyric acid (GABA) is the brains major inhibitory neurotransmitter. Studies have shown it is responsible for both the rise of growth hormone (when at rest) or the inhibition of growth hormone (when exercising).33-35 Oral GABA supplementation has increased growth hormone levels in humans. In one study, a single oral dose of 5 grams of gamma aminobutyric acid administered to 19 subjects significantly elevated plasma growth hormone levels compared to placebo-treated controls.36

33. Coiro V, Volpi R, Maffei ML, Caiazza A, Caffarri G, Capretti L, Colla R, Chiodera P. Opioid modulation of the gamma-aminobutyric acid-controlled inhibition of exercise-stimulated growth hormone and prolactin secretion in normal men. Eur J Endocrinol. 1994;131(1):50-5.

34. Rigamonti AE, Muller EE. Gamma-hydroxybutyric acid and growth hormone secretion studies in rats and dogs. Alcohol. 2000;20(3):293-304.

35. Vescovi PP, Volpi R, Coiro V. Alcoholism abolishes the gamma-aminobutyric acid (GABA)ergic control of GH secretion in humans. Alcohol. 1998;16(4):325-8.

This looks like a neat enough aspect of GABA supplementation in and of itself, the whole "ability to raise your GH secretion" thing that is, but I can't find a ton of studies demonstrating efficacy as a sleep aid.


T. L. Perry, Shirley Hansen
Abstract— The contents of GABA, homocarnosine, and β-alanine can be raised in rat brain for long periods of time by the continued administration of phenelzine, aminooxyacetic acid (AOAA), or isonicotinic acid hydrazide (INH). These 3 compounds apparently act by preferential inhibition of the enzyme GABA aminotransferase (GABA-T). Oral administration of phenelzine (20 mg/kg per day) caused a 25–50 per cent increase in GABA levels in rat brain, but produced appreciable toxic side effects. A similar increase in GABA levels in brain resulted from oral administration to rats of INH in a dosage of 60 mg/kg per day, without production of any obvious toxic effects. Simultaneous administration of large doses of pyridoxine did not abolish the GABA-elevating effect of INH. Brain GABA levels in the rat were increased by approx. 50 per cent by daily injections of AOAA (2.5 mg/kg per day). At this low dosage, AOAA injections in rats could be continued for at least 6 weeks without producing evident toxic effects. Oral administration of large amounts of GABA, on the other hand, failed to increase the content of GABA in the brains of rats not treated with GABA-T inhibitors, and failed to produce any further increase of brain GABA levels in rats treated with AOAA..

The Interaction Between GABA and Dopamine: Implications for Schizophrenia
James C. Garbutt and Daniel P. van Kammen
"...Although it was originally thought that GABA might be useful in treating schizophrenia because of its inhibition of dopaminergic activity, recent data have shown that in certain models GABA has the opposite effect on dopaminergic functions. Regardless of the relationship of GABA to dopamine, neither biochemical nor pharmacological studies have been able to demonstrate a clear and reproducible GABA disturbance in schizophrenia..."

How does the first study on GH and the following study correlate?

GHRH and sleep.
Obal F Jr, Krueger JM.
Department of Physiology, A. Szent-Györgyi Medical Center, University of Szeged, 6720, Szeged, Hungary. obal@phys.szote.u-szeged.hu
Suppression of endogenous GHRH (competitive antagonist, antibodies, somatostatinergic stimulation, high doses of GH or insulin-like growth factor) results in sA significant portion of the total daily growth hormone (GH) secretion is associated with deep non-REM sleep (NREMS). GH secretion is stimulated by the hypothalamic neurohormone, GH-releasing hormone (GHRH). Exogenous GHRH promotes NREMS in various species. imultaneous inhibition of NREMS. Mutant and transgenic animals with a defect in GHRHergic activity display permanently reduced NREMS which cannot be reversed by means of GH supplementation. GHRH contents and mRNA levels in the hypothalamus correlate with sleep-wake activity during the diurnal cycle and sleep deprivation and recovery sleep. Stimulation of NREMS by GHRH is a hypothalamic action. GABAergic neurons in the anterior hypothalamus/preoptic region are candidates for mediating promotion of NREMS by GHRH. In contrast to NREMS, stimulation of REMS by GHRH is mediated by GH. Simultaneous stimulation of NREMS and GH secretion by GHRH may promote adjustment of tissue anabolism to sleep.
PMID: 15336237 [PubMed - indexed for MEDLINE]

BTW, I keep seeing sources citing dosages of 200 MG three times daily; is taking such an excessive dosage, daily possibly, wise? Can you possibly, since your resting using this supplement, increase your GH uncomfortably high? (I'm ignorant)

GH stimulates the production of another chemical called insulin-like growth factor-1 (IGF-1) by the liver and by many body tissues.

HGH Increases Inflammation
Human growth hormone consists of several distinct -- but similar -- chemicals. Scientists refer to these distinct substances by their molecular weight. Each type of growth hormone appears to have unique properties, according to a June 2010 report in the "International Journal of Pediatric Endocrinology." The 22 kilodalton chemical often causes side effects such as swelling. An investigation published in the 2004 volume of the "Journal of Clinical Endocrinology and Metabolism" determined whether the 20 kilodalton chemical produced adverse events as well. Patients with growth-hormone deficiency received daily injections of HGH for four months. This treatment increased IGF-1 and insulin. It also increased lean body mass. Many patients, however, experienced swelling in their arms and legs.

HGH Causes Joint Pain
People infected with the human immunodeficiency virus have difficulty maintaining their weight. Moreover, medications treating HIV often cause increases in body fat. Growth hormone can help resolve these issues, according to a July 2007 report in the "Scandinavian Journal of Infectious Diseases." Yet, the benefits of HGH may come at a cost. A paper in the November 2007 issue of "Clinical Therapeutics" reviewed studies testing the effectiveness of growth hormone in HIV patients. At least 30 percent of the participants in these reports experienced either muscle or joint pain during hormone therapy. Many patients also experienced diabetic symptoms such as elevations in blood sugar.
IGF-1 Elevates Blood Sugar

Insulin-like growth factor 1 also affects body composition. An anabolic hormone, IGF-1 stimulates muscle growth in laboratory animals. A July 2011 article in "Endocrinology" showed that injecting mice with IGF-1 increased their body size and muscle mass. The authors observed no evidence of IGF-1 toxicity in this report, but other studies have shown that the hormone causes unwanted side effects. A clinical trial offered in the 2007 volume of the "Journal of Clinical Endocrinology and Metabolism" tested the effects of replacement therapy with IGF-1 in children. Participants received twice daily doses of the hormone for several years. About half the kids experienced brief episodes of hypoglycemia. This elevation in blood sugar caused seizures in a few cases.

IGF-1 Causes Headaches
Unusually small children often develop health problems as adults. Genetic defects in the IGF-1 system might underlie short stature, according to a July 2011 report in "Hormone Research in Pediatrics." This finding suggests that IGF-1 might prove useful in increasing height. A study presented in the 2010 volume of the "Journal of Clinical Endocrinology and Metabolism" tested this hypothesis in children with low levels of IGF-1. Twice daily injections for a year significantly increased the patients' height. This treatment, however, also caused headaches in nearly 40 percent of the kids. Nearly 25 percent of the children also reported feelings of nausea.