For athletes who get shivery, jittery and nervous from ordinary caffeine, there’s now a new alternative available from online stores. It’s called theacrine, and according to the animal and sponsored human studies that we’ve read it works – without the side effects of caffeine. What’s more, it seems that theacrine is safe too.
The structural formula of theacrine – scientific name 1,3,7,9-tetramethyluric acid – resembles that of caffeine. The substance is found in the fruit and juice of the cupuacu [Theobroma grandiflorum] and in kucha tea [Camellia assamica var. Kucha]. [Phytochemistry. 2002 May;60(2):129-34.] Theacrine is popping up in all sorts of bodybuilding supplements at the moment, especially in pre-workout and slimming products, and is promoted by manufacturers as having fewer side effects. The amount of theacrine per intake is usually somewhere in the range of 100-300 mg.
Theacrine versus caffeine
In doses of several tens of milligrams or several hundred milligrams, both theacrine and caffeine have a stimulatory effect. [J Asian Nat Prod Res. 2007 Sep-Dec;9(6-8):665-72.] [Pharmacol Biochem Behav. 2012 Aug;102(2):241-8.] Both substances also work in approximately the same way: they block the adenosine receptor and also boost the concentration of dopamine in the brain.
You usually find theacrine in supplements in combination with other stimulatory substances. Theacrine can reinforce the effect of these substances because it increases their solubility and therefore also their absorbability. Caffeine does the same, but theacrine does this five times better. [Mutat Res. 1977;39(3-4):297-315.]
Purus Labs puts theacrine together with caffeine, citrus extract and rauwolscine in TheaTrim. In 2015 a human study was published which showed that this supplement didn’t improve the subjects’ mental performance but it did help them to feel more energetic. [Nutrients. 2015 Nov; 7(11): 9618–9632.]
If you extrapolate the results of animal studies to humans, it seems that theacrine, unlike caffeine, in the doses you find in bodybuilding supplements has a painkilling effect. [Fitoterapia. 2010 Sep;81(6):627-31.]
Another difference between theacrine and caffeine is that, after a week, caffeine supplementation begins to lose its effect. As we mentioned above, caffeine works by sabotaging the adenosine receptors. Adenosine is a substance that tells cells to calm down. Administration of adenosine induces the body to make more adenosine receptors, which in turn reduces the stimulatory effect of caffeine. Somehow or other this doesn’t happen in animal studies where theacrine was administered instead.
Researchers at the private Center for Applied Health Sciences published the abstract of a small human study in 2014. In this study half a dozen subjects took 200 mg theacrine daily for a week. [J Int Soc Sports Nutr. 2014; 11(Suppl 1): P49.] The study was financed by Compound Solutions, [compoundsolutions.com] a producer of sports supplements. One of Compound Solutions’ products is the synthetic theacrine preparation TeaCrine.
The supplement continued to have an effect throughout the period of the experiment. It seems that the subjects’ bodies did not get used to it, as would have happened with caffeine. Up to six hours after intake the subjects reported feeling less fatigue, less stress, more libido, more inclination to do training, more concentration and more energy.
In comparable studies where the subjects were given caffeine, after a few hours there was a rebound effect, where subjects sometimes report feeling distinctly off colour. This doesn’t seem to happen with theacrine.
In January 2016 a study on the effect of supplementation with 200 and 300 mg theacrine daily – also funded by Compound Solutions – was published in the Journal of the International Society of Sports Nutrition. [Journal of the International Society of Sports Nutrition (2016) 13:2.] The study lasted eight weeks and the main focus was to determine the safety of theacrine.
The researchers found no indications that theacrine was dangerous to the liver, the immune system or the cardiovascular system. It also had no effect on body composition.
T1 = before supplementation, T2 = after 4 weeks’ supplementation, T3 = after 8 weeks’ supplementation; PL = placebo, LD = 200 mg theacrine per day, HD = 300 mg theacrine per day.
As the figures above show, theacrine supplementation did not lead to a reduction in fat mass. So the results of this study might raise doubt about the use of theacrine in slimming supplements. It seems that the substance is more suitable for pre-workout products.
The effects of TeacrineTM, a nature-identical purine alkaloid, on subjective measures of cognitive function, psychometric and hemodynamic indices in healthy humans: a randomized, double-blinded crossover pilot trial
Aside from caffeine, there is a relative dearth of evidence regarding natural ingredients that enhance subjective “energy” levels. We have studied a unique, naturally occurring purine alkaloid, present in Camellia assamica variety kucha tea (amongst other botanical sources) that acts on both adenosinergic and dopaminergic pathways that appears to influence multiple neurochemical pathways. As a first step in a series of experiments, we examined the effects of TeaCrine™, a nature-identical, chemically equivalent bioactive compound known as theacrine (1,3,7,9-tetramethyluric acid), in humans.
Using a randomized, double-blinded, within-subject (crossover) design, 15 healthy subjects (mean ± SD age, height, wgt, BMI: 28.3 ± 6.1 y, 175.7 ± 11.5 cm, 89.8 ± 21.7 kg, 29.1 ± 4.7) volunteered to ingest 200 mg of TeaCrine™ (Compound Solutions, Inc., Carlsbad, CA) (TC) or Placebo (PLA). Anchored VAS questionnaires were used to detect changes in various aspects of physical and mental energy and performance; side effect profiles, hemodynamics and biochemical markers of safety were also collected over a 3-hr post-dosing period. A subset of 6 subjects underwent a separate 7-day, open-label, repeated dose study comparing 100 mg, 200 mg and 400 mg of TC. Consent to publish the results was obtained from all participants.
The 200 mg dose of TC caused significant improvements in energy (TC: +8.6% vs. PLA: -5.7%, P=0.049) and reductions in fatigue (TC: -6.7% vs. PLA: +5.8%, P=0.04). A trend for improved concentration was also noted (TC: +2.4% vs. PLA: -1.3%, P=0.07). No changes in systemic hemodynamics or side effect profiles were noted. The N=6 cohort study demonstrated moderate to large effect sizes (0.50 to 0.71) with the 200 mg dose of TC over a 7-day period of assessment for the following subjective measures: energy, fatigue, concentration, anxiety, motivation to exercise and libido.
These preliminary data support the benefits of acute TeaCrine™ supplementation on subjective “energy” levels and some indices of mental performance. Future studies are underway to confirm these neurotropic effects and also explore potential benefits of TeaCrine™ on objective measures of cognitive and physical performance, inflammation, pain perception, and functional capacity.