Pre Workout Stimulants 101
If you want to know how your favorite pre workout stimulants boost energy and increase focus, this is the article for you!
What’s not to love about pre workout?
They infuse your mind and body with energy, focus, and motivation all the while igniting a cascade of catecholamines that power you through the most daunting of workouts. They also contain compounds to enhance performance, power output, and stamina, helping you achieve gains like never before.
They also tend to taste pretty damn good too.
So basically, pre workouts are awesome.
Yet, as awesome as pre workouts are, most of you reading this have little to no clue how exactly the various stimulants in pre workouts do what they do.
And, with that, we begun our discussion of today’s topic — an introduction to….
Pre Workout Stimulants
It’s the most widely consumed drug in the world and is naturally occurring in many common foods including coffee, tea, cocoa, and guarana seed. Due to our never-ending demand for more and more energy, caffeine is even being added to numerous everyday foods, including protein powder and even peanut butter!
So, how does caffeine do what it does?
Caffeine functions first and foremost as an adenosine receptor agonist. Adenosine is purine nucleoside that binds to adenosine receptors in the brain, causing a slow down in nerve cell activity. This results in your feeling tired and fatigued.
Caffeine readily crosses the blood-brain barrier (BBB) to “elbow out” adenosine, and in the process leads to greater energy and alertness.
On top of that, caffeine also prompts a strong increase in dopamine production. Dopamine is the primary neurotransmitter in the body affecting mood, motivation, and decision-making. With greater levels of dopamine, you’re more motivated to get in the gym and crush your workout.
Finally, caffeine also delivers some performance benefits as well, as it increases fatty acid oxidation, reduces neuromuscular fatigue, and improves stamina and strength.[2,3]
When you take all of those benefits into account, it’s no wonder why caffeine is the pre workout stimulant.
Up next, is another incredibly popular pre workout stimulant in synephrine. Naturally occurring in Citrus Aurantium (bitter orange), synephrine is a prominent beta-2 adrenergic receptor agonist)[4,5] and CNS stimulant. It’s structurally similar to ephedrine, but much safer for human consumption, and not too mention legal for use in supplements as well!
As a beta-2 receptor agonist, synephrine stimulates lipolysis, which liberates stored fatty acids from adipose tissue, freeing them up to be burned (“oxidized”) for energy. The benefit of this, is that when taken pre workout, synephrine helps you to burn fat for fuel early in your workout, sparing your glycogen stores for the really intense work later on in your training session, when you need it most.
Additional research has noted that synephrine increases energy expenditure, fat oxidation, and weight loss, which are some of the main reasons you’ll find this popular pre workout stimulant also included in fat burners, including Condemned Labz Arsyn.
As an added benefit, there’s even some research to show that using synephrine prior to exercise can enhance performance and reduce the onset of fatigue.
Found alongside synephrine in bitter orange is another CNS stimulant and beta adrenergic receptor agonist in hordenine.
Similar to synephrine, hordenine can stimulate lipolysis for enhanced fatty acid availability during training, but where hordenine really brings added value to a stimulant blend is its role as an MAO inhibitor.
MAO is an enzyme that degrades monoamines, such as dopamine, adrenaline, and noradrenaline. By inhibiting MAO, hordenine helps these powerful neuro-chemicals to hang around longer in the body, leading to greater energy, motivation, and focus during training.
Finally, hordenine also serves as a noradrenaline reuptake inhibitor which prevents noradrenaline (norepinephrine) from being reabsorbed in the body.[8,9] This again increases the amount of time you feel amped up and ready to unleash seven kinds of hell on the iron.
Also known as norcoclaurine, higenamine is a popular pre workout stimulant that came to the forefront when the FDA banned ephedrine alkaloids. Naturally found in Nelumbo Nucifera and Nandina plants, higenamine is yet another beta adrenergic receptor agonist that’s often considered a “weaker ephedrine.”
Due to its ability to stimulate the central nervous system and agonize beta-2 adrenergic receptors,higenamine is typically found in pre workouts designated more for fasted cardio as well as thermogenic fat burners. But, that’s not all, as higenamine also acts as a bronchodilator, which relaxes and opens airways, allowing for easier breathing during exercise.
Continuing on with our list of the best pre workout stimulants, we have the powerful energy enhancer and fat burning ingredient Yohimbine.
Derived from the Pausinystalia yohimbe tree, yohimbine is a strong CNS stimulant and alpha adrenergic receptor antagonist.
What exactly does that mean?
Well, your fat cells have both alpha and beta receptors.
Without getting too much into the complex physiology of fat loss, the important thing to konw is that beta receptors accelerate fat loss and alpha receptors for all intents and purposes, inhibit fat loss.
Now, when your body releases catecholamines (i.e. adrenaline, noradrenaline), they can dock at either the alpha receptors or the beta receptors. Ideally, we want these catecholamines to dock on the beta receptors, allowing for greater fatty acid availability and utilization for energy. But, this isn’t an ideal world, so sometimes these compounds bind to the alpha receptors, which essential turns fat burning “off”.
Yohiming, acting as an antagonist, binds to the alpha receptors allowing the fat burning catecholamines and hormones to bind to your beta receptors, liberating fatty acids to be burned for energy.
In other words, yohimbine prevents the alpha receptors on your fat cells from restricting fat burning.
Additionally, yohimbine also helps reduce appetite, spotlighting another reason it’s such a prominent fat burning supplement.
When used in pre workouts supplements, yohimbine gives an “edgy” aggressive feel to the energy boost, unleashing the inner beast buried deep down inside of you. It also stimulates noradrenaline (norepinephrine) release in the brain, leading to a tremendous surge in energy and focus.
One last note regarding yohimbine, to get the most fat burning potential from it, you need to take it on an empty stomach, as any elevation of insulin negates its pro-fat loss benefits,though if you just want the energy boost it gives, having some food in your system is fine.
Last, but certainly not least, in our laundry list of the best pre workout stimulants is 2-aminoisoheptane. It functions as a psychoactive central nervous system stimulant with a molecular structure resembling those of now banned pre workout stimulants in AMP Citrate, Ephedrine, and the ever popular DMAA.
Originally developed as a nasal decongestant for the treatment of bronchitis, 2-aminoisoheptane has emerged as a powerhouse pre workout stimulant for its ability to increase the uptake of dopamine and noradrenaline — two powerful neurotransmitters that heighten mood, motivation, and alertness.
Additionally, 2-aminoisoheptane has also been found to increase the pain threshold, allowing you to train harder and tolerate more pain during training before ending your set.
Convict Stim — THE Pre Workout Stimulant
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Bolstered by 300mg pure caffeine anhydrous and a cavalcade of other powerful stimulants, Convict Stim will ignite your senses and set your mind ablaze, ensuring your have the mental and physical energy, stamina, and focus dominate your workouts and get those gains.
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- Goods PSR, Landers G, Fulton S. Caffeine Ingestion Improves Repeated Freestyle Sprints in Elite Male Swimmers. Journal of Sports Science & Medicine. 2017;16(1):93-98.
- Hodgson AB, Randell RK, Jeukendrup AE. The Metabolic and Performance Effects of Caffeine Compared to Coffee during Endurance Exercise. Earnest CP, ed. PLoS ONE. 2013;8(4):e59561. doi:10.1371/journal.pone.0059561.
- Sidney J. Stohs, Harry G. Preuss, and Mohd Shara, “A Review of the Receptor-Binding Properties of p-Synephrine as Related to Its Pharmacological Effects,” Oxidative Medicine and Cellular Longevity, vol. 2011, Article ID 482973, 9 pages, 2011. doi:10.1155/2011/482973
- Stohs SJ, Preuss HG, Shara M. A Review of the Human Clinical Studies Involving Citrus aurantium (Bitter Orange) Extract and its Primary Protoalkaloid p-Synephrine. Int J Med Sci 2012; 9(7):527-538. doi:10.7150/ijms.4446.
- Ratamess NA, Bush JA, Kang J, et al. The effects of supplementation with P-Synephrine alone and in combination with caffeine on resistance exercise performance. Journal of the International Society of Sports Nutrition. 2015;12:35. doi:10.1186/s12970-015-0096-5.
- Frank M, et al; Hordenine: pharmacology, pharmacokinetics and behavioural effects in the horse; Equine Vet J. (1990)
- Barwell C.; School of Pharmacy; “Deamination of hordenine by monoamine oxidase and its action on vasa deferentia of the rat;” 1989
- Nedergaard O.; British Journal of Pharmacology; “Action of various sympathomimetic amines on the isolated stripped vas deferens of the guinea-pig;” November 1968
- Park, C; “Effects of higenamine on isolated heart adrenoceptor of rabbit”; Arch Int Pharmacodyn Ther. 1984 Feb;267(2):279-88
- Bai G, et al. Identification of higenamine in Radix Aconiti Lateralis Preparata as a beta2-adrenergic receptor agonist1. Acta Pharmacol Sin. (2008)
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