Blood Brain Barrier and Neurotransmitter Supplementation
Things that pass readily through the BBB are either small, lipophilic (non-polar) and/or a gas. By lipophilic we mean items that tend to mix with oils. Examples of some common molecules that can easily cross the BBB are caffeine, nicotine, heroin, valium, and CO2.
GABA and Phenibut
The inhibitory neurotransmitter, polar GABA is reported to have trouble getting across the BBB. A couple of non-prescription modifications can get GABA into the brain better. The first is called phenibut or beta-phenyl-GABA. Phenibut is basically GABA with a 6-carbon ring attached. This 6-carbon ring helps change the large, polar molecule into a large and less polar version, so it slips through the BBB. Once in the brain, the 6-carbon ring splits off and you get the GABA your brain needs. We like phenibut for occasional use and keep some in our house to help with sleep.
GABA and Picamilon
The other example is Picamilon or nicotinoyl-GABA. This is GABA with a vitamin B3 added. In the brain, the B3 and GABA are separated, and GABA can do its work. Picamilon is still available in Europe and Russia, but it is not readily available in the US at the time of this writing.
As mentioned, we have a decent amount of experience with phenibut. When used on an intermittent basis, it can be quite effective. We haven't used picamilon so can't comment from a personal point of view.
We used to carry phenibut but the FDA decided in all their convoluted wisdom that it can only be sold for research purposes. You can still find picamilon and/or phenibut if you do an internet search. At this time, we can't recommend any particular source.
GABA and Exercise
One twist to the GABA and BBB situation is the pituitary. Seems that GABA can get to the pituitary, and this is especially effective during exercise. In at least one study, taking GABA before exercise increased the production of HGH (human growth hormone) by over 400%. The dose used was 3g. Take your dose about 30 minutes prior to exercise to give it time to get working. You should notice the difference within a few days of using this routine. NuMedica GABA, link below!
Dopamine Example
Dopamine is an excitatory neurotransmitter that also doesn't get across the BBB very well. Taking dopamine can increase blood levels but not brain levels. The strategy here is to take supplements that help the brain process dopamine along with M. cochinchinensis seed extract purified to a high level of L-DOPA concentration. The brain can then make dopamine from the L-DOPA that does cross the BBB. This is the strategy behind Balance D and ExcitaPlus from NeuroScience.
What We Recommend
We often recommend phenibut to help increase GABA in the brain. This helps calm brain reactions to help lower anxiety and help with sleep.
ExcitaPlus or Balance D
We sometimes recommend things like ExcitaPlus and Balance D for symptoms of low dopamine like low motivation, low libido, fatigue and maybe movement disorders plus about a dozen other things. If you find that these dopamine enhancers are helpful, be sure to add a little serotonin support as increasing dopamine tends to lower serotonin. NeuroScience TravaCor is our usual go-to product for basic serotonin support.
