GABA, which stands for Gamma-aminobutyric acid, is a neurotransmitter that helps regulate communication between brain cells. It keeps the activity of nerve cells in check whenever neurons become “over-excited.” GABA is a crucial piece of the puzzle in your mood, cognition, and how your body responds to stress.
Much research links low levels of GABA in the brain to anxiety, depression, and various types of insomnia. It then makes sense that anyone who suffers from any of these disorders needs to increase their levels of GABA. And what better way to do it than with one of the many available GABA supplements.
Sounds simple in theory, but in practice, there is little evidence that this approach is effective.
The Blood-Brain Barrier
The reason why taking GABA supplements is not very effective is that, while they will increase the levels of it in the blood, circulating Gamma-aminobutyric acid does not pass the blood-brain barrier.
In other words, having increased levels of GABA in the blood stream does next to nothing to address the cause of the problem: not having enough of it in the brain.
Fret not, however. While the GABA pills you find in the supplement aisle of your local store may not be much help, other solutions exist. There are both prescription and non-prescription GABA derivatives and certain non-GABA supplements that do cross the blood-brain barrier.
All can very effectively reduce anxiety, help you think and improve your mood.
But first, let’s talk a little about that seemingly impenetrable wall, the blood-brain barrier. Its purpose is to limit what can cross over from your bloodstream to the central nervous system and to make sure certain substances never reach your vital brain tissues.
Not welcome are bacteria and all sorts of toxins. And, unfortunately, neither is the supplemental GABA you just ingested.
The brain likes to keep tight control over its levels of GABA. It prefers to make its own rather than to bring it in from outside sources, and the blood-brain barrier is its enforcer.
The brain will also strictly limit how much Gamma-aminobutyric acid it has. A 2001 study published in the “Journal of Neurochemistry” shows how GABA can be transported out of the central nervous system and back into the bloodstream using a special one-way back door .
Thankfully, as is the case with many seemingly impenetrable fortresses, they often are not. Where there is a will to get through there is a way.
Science has created several GABA-like drugs and supplements, also called derivatives or analogs, that function just like GABA in the brain, and that the blood-brain barrier will let pass.
Some of these analogs are prescription only. Commonly used ones include Gabapentin and GHB.
Gabapentin straight up increases GABA levels in the brain, though it is not entirely understood how it works . This drug is usually prescribed as a treatment for epilepsy and neurotic pain.
GHB, which stands for gamma-hydroxybutyrate, is the other well-known prescription GABA analog . It is available under the brand name Xyrem as a narcolepsy treatment and carries the generic name sodium oxybate.
There are also two popular non-prescription GABA derivatives that can cross the blood-brain barrier. Both are a bit like GABA in disguise.
The first is called Phenibut, or beta-phenyl-gamma-aminobutyric acid HCl (say that fast three times). It is pretty much GABA with a 6-carbon ring added to it. The extra carbon (the disguise) is enough to make the blood-brain barrier look the other way and let the supplement through.
Once it’s in, Phenibut acts on same receptors as naturally produced GABA, resulting in very similar effects.
The other supplemental GABA derivate is Picamilon. Sometimes called nicotinoyl-GABA, it too disguises itself. In this case, added to the GABA molecule is Vitamin B3. This combination is also allowed to cross the blood-brain barrier.
After Picamilon makes it into the brain, the Vitamin B3 simply goes away, leaving nothing but pure GABA behind. Unfortunately, Picamilon is next to impossible to find these days.
Other than prescription and non-prescription GABA derivatives, there is a third option. You can use other supplements allowed through by the blood-brain barrier which have nearly identical effects to increasing GABA levels in the brain. These supplements are called nootropics.
In fact, our friends Phenibut and Picamilon can be considered to fall into this category as well.
Nootropics are traditionally used to improve a variety of cognitive functions like memory, focus, clarity of mind, and thinking. But, several brain enhancing nootropic supplements, including the popular product Mind Lab Pro, can also reduce anxiety, improve mood, decrease stress and help with sleep.
Sound familiar? Those are all effects associated with increasing the levels of GABA in the brain.
Most importantly, nootropics will work significantly better than any GABA pills, which, as we have learned, don’t really work at all.