PharmaGABA®: Unparalleled Innovation for Unparalleled Performance

by | Dec 16, 2020 | 0 comments

Q : First Endurance has added an ingredient called PharmaGABA® to EFS-PRO. Why? What does it do for me?

A: Research shows the brain plays a significant role in fatigue and exercise tolerance. Our latest formulations of EFS and EFS-PRO expand the focus beyond simply supporting your body to buttressing up mental toughness—often the final hurdle an athlete has to overcome whether they’re training alone or competing.

Toward this end, our research has led us to ingredients like Suntheanine® (which we also include in EFS) and, in EFS-PRO, Suntheanine® plus PharmaGABA®. The net result of these two ingredients is to boost calm control while your body’s suffering is triggering panic in your brain. By balancing your brain’s response to suffering, EFS and EFS-PRO help ensure you get the most out of every stride or pedal stroke when the suffering ramps up and every watt is invaluable.

Many athletes don’t realize the brain plays a key role in endurance.

What is PharmaGABA®?

PharmaGABA® is a patented, fermented form of the oddball amino acid GABA (gamma-Aminobutyric acid). As its full designation suggests, GABA is a gamma amino acid, meaning the amino group is further away from the acid group. Though it is an amino acid, it’s not like the alpha amino acids that make up our proteins; however, just because GABA is not used in proteins does not mean it’s unimportant. GABA is your brain’s major neurotransmitter, and it’s also found all over your body, connecting your brain to other physical areas. This is a relatively new learning, so most of the preceding research literature on GABA begins with a flawed premise: that GABA ingested orally has no effect on the brain. Before these new findings, we were a wrong-way rabbit going down a badger hole, thinking it’s a rabbit hole. Never comes out alive.

What does it do?

The GABA supplied by PharmaGABA® is a major neurotransmitter that your brain uses to balance out stress and—in the context of endurance athletics—control the Central Fatigue that can force you to stop pushing before you’re physically unable to do so. It sharpens your mental edge and the surgeon’s calm needed to apply that edge with precision.

You may have read about Central Fatigue in our explanations of Suntheanine® (a patented type of L-theanine) that we added to EFS & EFS-PRO. We recommend reading that to see how and where GABA fits in to keep you mentally tough, pushing back Central Fatigue (your brain telling you to stop torturing yourself); however, we’ll provide a short refresher here in case you missed the theanine blog.

GABA is quantitatively the most important neurotransmitter in your brain. It’s the stop-and-think, anti-stress agent in your brain chemistry, and it serves to counterbalance glutamate, the excitatory agent, in order to balance the stress of the latter with the calm control of the former. In short, GABA keeps your brain balanced, so you can shrug off stress and the pain-induced panic that make you dial back your efforts during high-stress, high-output moments in races or training sessions. It’s less about shushing your screaming legs and more like you don’t even hear the voice shouting “STOP” at all.

PharmaGABA® allows endurance athletes to push their perceived maximal exertion closer to their true maximal exertion for a longer period of time.

How does it work?

We’ve been dwelling in brain chemistry for some time now, but here’s where we reveal that a funny thing happens to GABA when taken orally and even when given intravenously: It does not really get into the brain, at least not like theanine does. Much research finally found that a tiny amount of exogenous GABA might sneak into the brain via the hypothalamus, which intentionally lets in a few signaling molecules (GABA included), in order to know which hormones to make or break. But we don’t care about whether oral GABA gets into the bloodstream and brain.

Despite many wags bashing poor oral uptake of GABA into the brain as pointless for supplementing GABA, we know GABA administered orally can affect the brain, and newer research on GABA has finally figured out how and why it works orally. The expression “gut feeling” is one way to describe it, as oral GABA operates through your gut. It never leaves the gut to get into the bloodstream, at least not enough to feed your brain, but the GABA you consume does augment the GABA naturally produced by your gut, and your bellyful of GABA sends a calming signal directly to your brain to be more receptive to the effects of the GABA already in your brain, keeping its antagonist, glutamate, in check.

Oral GABA signals your brain via the extensive networks of nerves that make up the gut-brain axis. GABA triggers your gut absorptive cells to secrete microRNA signals to the adjacent nerves, in a communication pathway newly found and unsuspected. So PharmaGABA® in EFS-PRO is an additional antistress, calm-but-alert boost for your brain that makes your inhibitory neurotransmitter system more effective at balancing out the excitatory system.

Dose?

As with L-theanine, our review of clinical research finds that the key to administering GABA for exercise performance is simple: more often, not more. Studies using higher and higher doses of oral or intravenous GABA demonstrate less efficacy than smaller doses. In fact, too much GABA in a single, excessive dose (100 mg and up) can make you dull and lazier mentally, imbalancing your brain’s response to stress and causing less alertness—ultimately offsetting the neurotransmitter balance we’re trying to maintain. To prevent that self-defeating overdose, we match the doses used in human studies for biological effects; taking this amount (17 mg) every 30 minutes keeps gut GABA levels in the sweet spot of balancing your brain.

Why PharmaGABA®?

We insist on using only patented, clinically-studied PharmaGABA® because it’s the specific type of GABA that demonstrates the strongest evidence that oral GABA is effective in human studies. And we know why that is. In a word: Conformation. Conformation is the dreaded C word of chemistry, a very important, nebulous-but-always-present, little-known fact about GABA, amino acids, and a lot of other compounds in our bodies that involves crazy molecular-bonds chemistry—something even chemists try to avoid.

Simply put, because each atom-to-atom bond in GABA can rotate freely, the exact shape of every molecule in your body is constantly changing—and changing A LOT. Molecular shape depends on which of the pieces of the molecule (GABA in this case) are too close to each other during the inevitable spinning, and that spinning can sometimes get the molecule stuck in a spring-loaded, tense shape. Most compounds do this—even glucose itself is a poster child of molecular conformation variations—but conformation can confound the receptors looking for specific molecular shapes to bind with. Receptors are like a lock and key that depends on an electrical fit rather than a mechanical, and conformation determines the compatibility of that union.

GABA made via chemical synthesis is born in harsh conditions, and those conditions can affect conformation, pushing some or all of the GABA molecules into slightly twisted, distorted shapes that don’t fit into the receptors’ locks as well as they should. So even though the molecule produced is chemically verifiable as GABA, those conformational changes can make molecules act completely different, electrically. The net result is usually less effect of the molecule-receptor signal. In other words, GABA made synthetically can look, smell, sound, feel, and quack like real, natural GABA, but it lays an egg in the receptor. In fact, taking 100 or 500 mg or more of chemically synthesized GABA can short-circuit or be contrary to GABA actions, which helps explain why a lot of GABA human studies do not find effects. Confounded Conformation!

Instead of chemical synthesis, PharmaGABA® is made by enzymes via microbial (Lactobacillus species) fermentation, a process that produces the same conformation as the GABA your body makes naturally—which, incidentally, is also made by similar enzymes. The result: PharmaGABA®’s key is the same shape as endogenous, naturally occurring GABA, so it fits neatly into the locks on your body’s receptors. Testing for molecular conformation is not easy and not routine and seldom done commercially, but since PharmaGABA® addresses the risk of ill-fitting conformation, it ensures that EFS-PRO’s GABA boost isn’t just blunted or discarded as a useless, broken tool by your body.

So now you have the bare bones of why we added Suntheanine® to EFS and EFS-PRO, and PharmaGABA® to EFS-PRO. We use what your body is looking for and can utilize efficiently. Balance your brain; balance your control.

Your brain uses changes in neurotransmitters to actually turn down nervous impulses for muscular contraction during fatiguing exercise (like serotonin, for example). Suntheanine® and PharmaGABA® balance neurotransmitters in a way to prevent fatigue by calming your built-in panic mode.

What makes you bonk after long, hard exercise?

Is it your muscles? Not enough antioxidants? Too much lactate? Not enough carbs or fat for fuel?

Your joints, tendons, ligaments screaming? Pain? Your brain saying ENOUGH!?

Turns out it is all of the above. But your brain makes the final decision that shuts down nerve impulses to muscles.

Keeping your brain in the game keeps you running.
(Dr. Luke-ism)

How to Maximize Benefits With EFS-PRO
(Suntheanine® – 50 mg per Serving – and PharmaGABA® – 17 mg per Serving)

  • Dose: More often, not more.
  • Timing is everything.
  • Keep a steady blood/brain level of theanine and gut uptake of GABA as long as you need to, during exercise.
  • No adaptation – you can use it every day for many weeks or many days apart and it will have the same effects. 

Why We Added PharmaGABA® to EFS-PRO

  • Adds specific mental support for “mind over matter” during exercise.
  • Helps keep you clear-headed, alert, focused but calm and collected.
  • Antistress mental effects.
  • Helps with jitters/anxiety – helpful before and during exercise.
  • Supports a healthy immune system.
  • PharmaGABA® is the clinically-tested, effective form of GABA.
  • PharmaGABA® is not the same as chemically-synthesized (cheaper) GABA because of conformation.
  • Oral GABA works via interacting with the gut-brain nerve axis, not by getting GABA into the brain.
  • PharmaGABA® and Suntheanine® work together to help balance the calming and stimulating neurotransmitter systems in your brain to emphasize control, not overexcitement or being a dullard.
  • PharmaGABA® is the Right Stuff!

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