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Saturday, June 27, 2015

GABA-Transaminase Inhibitors (GABA-Reuptake Inhibitors) (How to Enhance GABA & Prevent it's Breakdown)



While monoamine neurotransmitters such as dopamine, serotonin and norepinephrine are metabolized (broken down, cleared & made useless) primarily by MAO enzymes and & COMT , amino acid transmitters which are much more abundant, are broken down by totally separate enzymes.


Additionally, transporters that take their respective neurotransmitters 'out of operation' as in DAT to dopamine, and SERT to serotonin, are structurally different than their amino acid transmitter counterparts.


GABA-T or GABA Transaminase; is the enzyme that transports GABA out of the synaptic cleft and acts as a 'SHUNT' (also referred to as the GABA shunt enzyme or shunt scenario), effectively diverting (or really sending away) active GABA currents. 

GABA-T, also known as 4-aminobutyrate transaminase is what DAT is to dopamine and SERT is to serotonin, it degrades neuronal GABA preventing it from accumulating and thus reaching a higher order of consistency.

Inhibiting the enzyme may lead to not only sustained GABA levels but also potentiation of all substances that act on the GABA system and thus inhibiting the enzyme will amplify the effects of alcohol and other depressants.

There are a few Active and human compatible transaminase inhibitors that may enhance the activity of GABA and thus prolong it's effects.

Natural GABA transaminase inhibitors (GABA Reuptake Inhibitors) would be. 


  • Lemon Balm Extract (!) (!)
  • Rosemarinic Acid Extract (!).
  • Gastrodin (!)
**Gastrodin is a known neuroprotective agent which is primarily marketed by Life Extension, a great deal of research has been conducted in the life extension community and by some practicing naturopathic doctors as well as UA researchers, however, it is not strictly a GABA-T inhibitor.**

~My recommended brands of each respective product are below~

Lemon Balm
              


ROSEMARINIC ACID EXTRACT w/ Butterbur
(helps anxiety, allergies and asthma)




Brand Name Gastrodin
("BRAIN SHIELD
")







Pharmaceutical Transmaninase Inhibitors

Vigabitrin; an anti-epileptic drug marketed as Sabril

Vigabatrin, a GABA Transaminase Inhibitor, Reversibly Eliminates Tinnitus in an Animal Model

Vigabatrin decreases cholecystokinin-tetrapeptide (CCK-4) induced panic in healthy volunteers.




****REFERENCES/CITATIONS/SOURCES****
The GABA shunt: an attractive and potential therapeutic target in the treatment of epileptic disorders.

Broad-Spectrum Protection Against Brain Aging : By Arlan Myerson

Gastrodin Discussion @ Longecity 

Use of inhibitors of gamma-aminobutyric acid (GABA) transaminase for the estimation of GABA turnover

Chronic administration of the antidepressant phenelzine and its N-acetyl analogue: effects on GABAergic function.

GABA-elevating effects of the antidepressant/antipanic drug phenelzine in brain: effects of pretreatment with tranylcypromine, (-)-deprenyl and clorgyline.

Vigabatrin, a GABA Transaminase Inhibitor, Reversibly Eliminates Tinnitus in an Animal Model


Vigabatrin decreases cholecystokinin-tetrapeptide (CCK-4) induced panic in healthy volunteers.








3 comments:

  1. Great article! I personally use rosemarinic acid and butterbur for both allergies and the gaba effects. Good stuff.

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  2. Hello,

    I've been taking Gastrodin as I am experiencing tolerance withdrawal from benzos and thought it might be useful. I am not sure that it is helping though, could it be possible that it is making withdrawals worse? I don't fully understand the mechanism of how it works in the brain in the same way as gaba agonists and antagonists.

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    Replies
    1. I doubt it would make it worse. It basically acts by causing more natural GABA to stay in the Brain longer (prolonging its activity by reversing the transport). You could try L-Theanine, Taurine and L-Lysine, that might do you the most good if you are withdrawing. Use Solgar and / or NutraBio brand if you are in the USA.

      Studies.

      --> https://www.ncbi.nlm.nih.gov/pubmed/16930802
      --> http://www.naturalhealth365.com/anxiety-brain-depression-taurine-1590.html
      --> https://www.ncbi.nlm.nih.gov/pmc/articles/PMC420386/

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