Loco: Behind the Label with Guerrilla Chemist

Loco by Myoblox is an ultra-premium, fully-dosed preworkout formula that centers around a balance of stimulants and nootropics with extreme blood-flow and increased performance. Loco has a whopping 17g of active compounds per full serving, including mega doses of betaine, taurine, and beta alanine, as well as a unique blend of powerful stimulants like N,N-dimethylphenylethylamine, synephrine, higenamine, choline and, of course 400mg of all-natural caffeine. This article will go into detail on the main active ingredients and how they help with exercise and performance.

Synephrine: A natural alkaloid from the plant Citrus aurantium, synephrine is a beta-2 adrenergic receptor agonist. Chemically, synephrine is similar in structure to ephedrine, the one of the strongest and most widely used stimulants ever. Synephrine has been shown in humans to increase basal metabolic rate (BMR), as well as the rate of lipolysis, the breaking down of fats into free fatty acids to be burned for energy.1  In one study, healthy participants taking 50mg of synephrine burned an extra 65kcal within 75min of consumption, which is why it's been used widely as a thermogenic and fat loss ingredient.2   There is also a nice synergistic response with the addition of caffeine, both in fat-burning and CNS stimulation, as well as being much safer than other phenylethylamine(PEA) compounds. Synephrine does not seem to cause a significant increase in blood pressure, vasocontrictiveness, or other cardiovascular side effects, even when combined with caffeine.3 Typical doses are between 25-50mg/d.

N,N-dimethylphenylethylamine: N,N-dimethyl phenylethylamine is a naturally occurring PEA(phenylethylamine) derivative found in the plant Eria Jarensis Ames.4 PEAs are stimulants that act as releasing agents for monoamines such as dopamine and norepinephrine. The euphoric effect from PEAs is from the release of dopamine. The biggest issue with PEAs is how quickly they are metabolized by monoamine oxidase-B(MAO-B). PEA has a half-life of approximately 5-10min. This is where N,N-dimethyl phenylethylamine has an advantage over other PEAs. As the name implies, the molecule has 2 bulky methyl groups attached to the amine group, which can delay the metabolism by MAO-B via steric hindrance. One study in mice and humans showed that N,N-dimethyl phenylethylamine still had activity in the brain at 60min.5 These methyl groups also make the molecule more lipophilic (fat soluble) which leads to greater ability to cross the blood-brain barrier. Unfortunately, there no studies to show its effects as a cognitive enhancing agent, but anecdotally as well as biochemically the increase in release of dopamine can elevate mood and focus. Typical doses are between 100-250mg/d.

Higenamine: Higenamine is an interesting and underused stimulant that is naturally found in many plant species, with Nelumbo nucifera being the most common. Structurally, higenamine is a combination of the amino acid L-tyrosine and the neurotransmitter dopamine, with the PEA backbone subtly hidden in the molecule. Higenamine is another beta-2 adrenergic receptor agonist that has a very quick onset time and reaches peak levels in <7 minutes, but also seems to have nootropic properties. Higenamine works by increasing levels of cyclic adenosine monophosphate (cAMP), a messenger molecule that has effects on glucose and fat metabolism, by activating the enzyme adenylate cyclase.6   This mechanism is similar to how caffeine works, and caffeine can even potentiate the production of cAMP, which leads to more free fatty acids in the bloodstream to be burned for energy. Like most beta-2 agonists, higenamine also has a bronchodilation effect, but more interestingly a strong vasorelaxation effect, which is not common among stronger stimulants.7   Its vasodilation effect can help was even strong enough to investigate the use of higenamine for erectile dysfunction. There is only one human study on higenamine, but it was combined with caffeine and yohimbine (The study did not list the amount of higenamine, but did list caffeine at 270mg). It did show a significant increase in calorie burning(around 1.5kcal extra burned per hour), calories burned from fat, circulating free fatty acids, and smooth muscle contraction force.8 Typical doses seem to be in the 25-75mg/d range.

Betaine Anhydrous: Betaine, also known as trimethylglycine, is a metabolite of choline and is naturally found in beetroot. Betaine acts as a methyl donor to either help eliminate harmful molecules like homocysteine or form S-adenosyl methionine (another methyl donor that helps make creatine endogenously). Homocysteine is a dangerous metabolite of the amino acid cysteine that increases significantly during exercise.9 Elevated levels of homocysteine have been attributed to endothelial cell damage, as well as a biomarker for cardiovascular disease and kidney failure. Research shows that using 3-6g of betaine can reduce homocysteine levels by 10% in healthy individuals to 20-40% in subjects with chronic elevated levels.10 Betaine is also an osmolyte (helps bring water into cells) that helps regulate cell hydration and tonicity, which seems to be the main mechanism for boosting performance. Betaine has many ergogenic benefits such as increased power and strength. A 2010 study involving 12 resistance-trained athletes were given either 2.5g/d of betaine or a placebo for 14 days and exercise performance was measured. The betaine group showed gains in bench throw power, isometric bench force, vertical jump power and isometric squat force.11 A 2011 study demonstrated that 14 days of betaine supplementation resulted in greater post-exercise muscle tissue oxygen saturation vs the placebo. The implications of this may be that betaine may have enhanced Kreb’s cycle efficiency due to its omsoprotective properties and may also improve high-intensity aerobic performance, especially in very hot environments. It stands to reason that betaine may also increase mitochondrial function and improve tissue oxygen consumption.12 Another benefit of betaine supplementation is increased blood flow via NO production. A small study involving 12 subjects who were given either 6g of betaine (the amount in Loco) or a placebo for one week showed a 185% increase in NO plasma levels (crazy pumps).13

Glycerol monostearate: Glycerol monostearate is the mono fatty acid form of glycerol, the three-carbon backbone of all fatty acids. Since glycerol is a liquid at standard temperature and pressure, the fatty acid stearic acid was added to make a powdered form of glycerol. Glycerol is a very powerful osmolyte that works by bringing water molecules into your cells to not only prevent dehydration but induce a state of hyperhydration.14   Exercise performance has been shown to decline with as little as 2% dehydration, and a 5% dehydration can negatively affect performance by 30%.15 A study where subjects were given a 20% glycerol solution 1hr prior to exercise showed at 24% increase in exercise time to exhaustion, as well as lower average heart rates.16 A 20-day study involving 40 subjects showed that consuming a glycerol/water drink improved both aerobic and anaerobic exercise performance vs consuming only water.17   Glycerol plus plenty of water is something that everyone should be taking prior to exercising to achieve maximum performance. Since glycerol is very safe, typical doses are a max of 120g/d, with 2-5g prior to exercise.

Beta Alanine: Beta alanine is an amino acid that is used in the body along with histidine to synthesize the pH buffer carnosine. Carnosine, which is largely found in muscle cells, protects muscles from exercise-induced damage due to excess lactic acid build-up. Lactic acid gives off acidic protons that can accumulate in your muscle cells as quickly as 4 minutes post exercise and prevent muscle contractions, inhibit phosphocreatine regeneration and glycolysis.18   Beta alanine is the rate-limiting step in carnosine synthesis. Increasing carnosine via beta alanine supplementation has been shown to decrease fatigue, increase workload, and increase time to exhaustion. According to most of the data, beta alanine exhibits its greatest affect in high-intensity, short duration bouts of exercise; from 60-240s.19   This seems ideal for intense weight training sets. Doses of 4-6g/d of beta alanine have been shown to increase muscle carnosine levels by 64% after 4 weeks and up to 80% after 10 weeks.20 Side note- the "tingling" feeling that beta alanine gives you is known as paresthesia and is caused by interactions between beta alanine and Mas-related genes and sensory nueron receptors on your skin. According to most studies, the saturation point where beta alanine is most effective seems to be 179g(built up over time). Typical doses of beta alanine are 2-6g/d.

My thoughts on Loco:

Loco was the first product I tried from Myoblox and I loved it. It's what got me into the brand and interested in their other products. To be fair, the first Loco I tried was the limited edition Magical Unicorn version, but I have since used a few different versions including the "normal" one. I love the large amounts of betaine and taurine, as well as the blend of stims with focus. Between the 6g of betaine and 2g of taurine, I definitely noticed less fatigue during training. I will say that I am glad to see Myoblox lowered the beta alanine dose from 5g to 4g, as it was a little much for me. Other than that, I think this is a very solid pre-workout formula that uses premium ingredients at copious doses. I'm very excited to try the new Loco Cinco!

- The Guerrilla Chemist

 

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References:

  1. Haaz, S., et al. "Citrus aurantium and synephrine alkaloids in the treatment of overweight and obesity: an update." Obesity reviews1 (2006): 79-88.
  2. Stohs, Sidney J., et al. "Effects of p-synephrine alone and in combination with selected bioflavonoids on resting metabolism, blood pressure, heart rate and self-reported mood changes." International journal of medical sciences4 (2011): 295.
  3. Seifert, John G., et al. "Effect of acute administration of an herbal preparation on blood pressure and heart rate in humans." International journal of medical sciences3 (2011): 192.
  4. Hedman, K; Studies on Orchidaceae Alkaloids. XV. Phenethylamines from Eria jarensis Ames.; Department of Organic Chemistry, University of Stockholm; October 14, 1969
  5. Shinotoh, Hitoshi, et al. "Kinetics of [11C] N, N-dimethylphenylethylamine in mice and humans: potential for measurement of brain MAO-B activity." Journal of nuclear medicine 28.6 (1987): 1006-1011.
  6. Kam, SC; Do, JM; Choi, JH; Jeon, BT; Roh, GS; Chang, KC; Hyun, JS (2012). "The relaxation effect and mechanism of action of higenamine in the rat corpus cavernosum". International Journal of Impotence Research. 24 (2): 77–83.
  7. Wong, KK; Lo, CF; Chen, CM (1997). "Endothelium-dependent higenamine-induced aortic relaxation in isolated rat aorta". Planta Medica. 63 (2): 130–2.
  8. Lee, Sang-Rok, et al. "Acute oral intake of a higenamine-based dietary supplement increases circulating free fatty acids and energy expenditure in human subjects." Lipids in health and disease1 (2013): 148.
  9. Herrmann, Markus, et al. "Homocysteine increases during endurance exercise." Clinical chemistry and laboratory medicine11 (2003): 1518-1524.
  10. Alfthan, Georg, et al. "The effect of low doses of betaine on plasma homocysteine in healthy volunteers." British journal of nutrition4 (2004): 665-669.
  11. Lee, Elaine C., et al. "Ergogenic effects of betaine supplementation on strength and power performance." Journal of the International Society of Sports Nutrition1 (2010): 27.
  12. Trepanowski, John F., et al. "The effects of chronic betaine supplementation on exercise performance, skeletal muscle oxygen saturation and associated biochemical parameters in resistance trained men." The Journal of Strength & Conditioning Research12 (2011): 3461-3471.
  13. Iqbal, Omer, et al. "Betaine induced release of tissue factor pathway inhibitor and nitric oxide: implications in the management of cardiovascular disease." The FASEB Journal4 (2006): A655-A655.
  14. Riedesel, Marvin L., Timothy P. Lyons, and M. Colleen Mcnamara. "Glycerol-induced hyperhydration." (1991).
  15. Barr, Susan I. "Effects of dehydration on exercise performance." Canadian Journal of Applied Physiology2 (1999): 164-172.
  16. Montner, P., et al. "Pre-exercise glycerol hydration improves cycling endurance time." International journal of sports medicine01 (1996): 27-33.
  17. Patlar, Suleyman, Hasan Yalçin, and Ekrem Boyali. "The effect of glycerol supplements on aerobic and anaerobic performance of athletes and sedentary subjects." Journal of human kinetics1 (2012): 69-79.
  18. Fitts, Robert H. "Cellular mechanisms of muscle fatigue." Physiological reviews1 (1994): 49-94.
  19. Hobson, Ruth M., et al. "Effects of β-alanine supplementation on exercise performance: a meta-analysis." Amino acids1 (2012): 25-37.
  20. Trexler, Eric T., et al. "International society of sports nutrition position stand: Beta-Alanine." Journal of the International Society of Sports Nutrition1 (2015): 30.

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