STIMULANTS

A stimulant is a substance that raises levels of cellular activity in the body. They are generally associated with nervous system excitement. When taken in optimal doses, stimulants make you feel invigorated, motivated, and focused. 

Caffeine 

Since caffeine is a well-documented central nervous system stimulant, then it is no surprise that it has profound positive effects on energy and focus (like most stimulants). Caffeine non-selectively blocks adenosine receptors. In the brain, adenosine binds to nerve cells and makes them slowdown in their activity. Caffeine is structured much like adenosine, so nerve cells readily allow caffeine to bind to their adenosine receptors, thus blocking the inhibitory action of adenosine on nerve activity. As such, the caffeinated brain is chock full of hyperactive nerve cells, an environment perceived by the pituitary as an emergency which results in adrenaline release from the anterior pituitary. As well, caffeine intake results in increased dopamine levels in the brain, giving the user a sense of well-being.

A meta-analysis published in the Scandinavian Journal of Medicine and Science in Sports showed that caffeine dampened perceived exertion during and after exercise by 5.6% compared with placebo [4]. Ingesting caffeine before a workout has been shown to significantly improve endurance in aerobic and anaerobic sports. It has been postulated that aerobic performances benefit from increased free fatty acid mobilization, thus improving time to exhaustion. However, for short duration anaerobic performances (like weight training) scientists speculate that the caffeine induced increase in dopamine signaling in the basal ganglia has the greatest effect on time to exhaustion. Nonetheless, all of this means that you can push harder and for longer by ingesting caffeine before training. 

As always, we recommend taking between 100-400mg in a single dose 30-60 minutes preworkout. Adjust dose based on tolerance and body mass. Remember, caffeine is a stimulant, so more is not always better. 

Reference:

• Doherty M, Smith PM. Effects of caffeine ingestion on rating of perceived exertion during and after exercise: a meta-analysis. Scand J Med Sci Sports. 2005 Apr;15(2):69-78.

Theacrine

Although theacrine was discovered way back in 1937 in tea leaves (Cameillia sinensis), it has been only recently introduced to the supplement world. Theacrine (l,3,7,9-tetramethyluric acid) is a special compound that shares a similar chemical structure to caffeine—thus it shares some of caffeine’s positive energizing effects. Theacrine is unique, however, in that it promotes improvements in energy and mood, but without over the stimulation—- or what we commonly refer to as “jitters”.

In recent years, it has been shown to have several interesting pharmacological properties, including anti-inflammatory and pain reliving action, antidepressant effects. Theacrine’s energizing effects are primarily due to its “caffeine like” actions— i.e., blocking adenosine receptors and inhibiting dopamine reuptake. As such, theacrine stacks very well with low doses of caffeine, and you get all the energizing benefits of both with little to no jitters. 

Look for theacrine in preworkout formulas or as a standalone energy booster. Although dosing guidelines are not well established, 100-200 mg taken 30-60 minute preworkout has been shown to improve fatigue, anxiety, energy, motivation to exercise, and concentration. NOTE: Theacrine is not sold on its own from VITAMIN SHOPPE, but it may be included in formulations (especially preworkout)— I forecast that by the time this is published Vit Shoppe will likely have a few theacrine products. However, If you want to take this section out, I am totally cool with that. 

Reference:

28

\\

• Kuhman DJ, Joyner KJ, Bloomer RJ. Cognitive Performance and Mood Following Ingestion of a Theacrine-Containing Dietary Supplement, Caffeine, or Placebo by Young Men and Women. Nutrients. 2015 Nov 19;7(11):9618-32. 

http://www.compoundsolutions.com/science.html

NOOTROPICS

Nootropics are commonly referred to as, “smart drugs”. This class of supplements improve brain function, memory, clarity, creativity, and focus. 

Alpha GPC (L-Alpha Glycerylphosphorylcholine)

Alpha-GPC is a choline-containing supplement that has been shown to be pharmacologically active at higher doses. Alpha-GPC supplementation increases choline levels in the brain and body much better than any other supplemental source of choline. 

Why boost choline levels? 

Choline has been an area of focus of many supplement studies concerned with human performance. Most of this research has focused on long duration exercise, as choline depletion is thought to play a role in fatigue [6]. Choline is a precursor to the production of acetylcholine (Ach), which a neurotransmitter responsible for producing the action potentials that stimulate a muscle to contract. Alpha-GPC is of interest for nootropic purposes, as it appears to have cognitive-enhancing properties and can decrease the rate of cognitive decline in the elderly [7]. Alpha-GPC has also been shown to enhance growth hormone production in young and older subjects [8]. 

As a brain booster, take 200-450 mg of alpha GPC, 3 times per day, with one dose 30-60 minutes before training and another immediately before bed.  

References:

• Marcus L, Soileau J, Judge LW, Bellar D. Evaluation of the effects of two doses of alpha glycerylphosphorylcholine on physical and psychomotor performance. J Int Soc Sports Nutr. 2017 Oct 5;14:39. 

• Scapicchio PL. Revisiting choline alphoscerate profile: a new, perspective, role in dementia? Int J Neurosci. 2013 Jul;123(7):444-9. 

• Ceda GP, Ceresini G, Denti L, Marzani G, Piovani E, Banchini A, Tarditi E, Valenti G. alpha-Glycerylphosphorylcholine administration increases the GH responses to GHRH of young and elderly subjects. Horm Metab Res. 1992 Mar;24(3):119-21.

Magnesium Threonate 

Magnesium is an essential macroelement, meaning that it must be acquired in the diet in relatively large amounts. It is known to help keep the heart beating regularly, it maintains bone health, and supports the immune system. Magnesium is involved in numerous processes that affect muscle function including oxygen consumption, energy production and electrolyte balance [9]. 

Magnesium deficiencies are common in North American diets, and this essential element is lost in sweat during exercise and when we urinate. Research shows that magnesium intake less than 260 mg/day for male and 220 mg/day for female athletes leads to magnesium deficiencies [10].  Athletes who restrict diet are especially vulnerable to an inadequate magnesium status. The relationship between magnesium status and exercise has received significant research attention. This research has shown that exercise induces a redistribution of magnesium in the body to accommodate metabolic needs. There is evidence that marginal magnesium deficiency impairs exercise performance and amplifies the negative consequences of strenuous exercise (e.g., oxidative stress). 

Magnesium threonate is a special form of magnesium that is easily transported across the blood-brain barrier to increase brain magnesium levels (11, 12). This is in contrast to most magnesium supplements that increase blood/body levels of this element, but change very little at the level of the central nervous system. This unique effect of magnesium threonate has been shown to improve synaptic density, which has been shown to improve cognitive performance [12, 13].  

If you are looking to give brain boosting magnesium threonate a try, we recommend taking 2000 mg in a single dose immediately before bed. This may seem like a large dose, but since it is a compound, this will yield 144 mg of elemental magnesium. 

References:

• Zhang Y, Xun P, Wang R, Mao L, He K. Can Magnesium Enhance Exercise Performance? Nutrients. 2017 Aug 28;9(9). 

• Nielsen FH, Lukaski HC. Update on the relationship between magnesium and exercise. Magnes Res. 2006 Sep;19(3):180-9. 

• Vink R. Magnesium in the CNS: recent advances and developments. Magnes Res. 2016 Mar 1;29(3):95-101.

• Sun Q, Weinger JG, Mao F, Liu G. Regulation of structural and functional synapse density by L-threonate through modulation of intraneuronal magnesium concentration. Neuropharmacology. 2016 Sep;108:426-39. doi: 10.1016/j.neuropharm.2016.05.006. 
• Slutsky I, Abumaria N, Wu LJ, Huang C, Zhang L, Li B, Zhao X, Govindarajan A, Zhao MG, Zhuo M, Tonegawa S, Liu G. Enhancement of learning and memory by elevating brain magnesium. Neuron. 2010 Jan 28;65(2):165-77.