Theacrine Supplementation

by on September 17, 2015


Theacrine: Caffeine’s Curious Cousin
By Alden Ryno

Knowledge is power” -Sir Francis Bacon”

The time has come again. The Mountain Dog has been toiling away in the depths of his lab. Formulating a product that will, once again, take the bodybuilding world by storm. He knows his stuff, and you know that. But now it’s for you to learn some of the stuff that he knows….

We love caffeine! That is until we get the jitters. Until we crash. Until our adrenals get fried. There must be an alternative… Perhaps something with a cleaner, smoother experience leaving us in control.

Thankfully, nature is quite crafty and there is an alternative. Enter theacrine (TeaCrine®).

Like caffeine, theacrine is a member of a group of natural compounds called purines (Figure 1). Purines are found in all kinds of plants and afford us with a variety of benefits, as seen with caffeine and as we’ll discuss further with theacrine.

theacrine
Figure 1:
Chemical structure of purine.

First, I’d like to demonstrate the structural differences between caffeine and theacrine. While these differences may appear relatively insignificant, I’d like to mention that even the three dimensional orientation of atoms in space can drastically alter how our bodies metabolize compounds. Heck, a single carbon atom and two hydrogen atoms differentiate formic acid and acetic acid. The former, found in ant venom, will likely kill you upon ingestion. The latter, when diluted, is used as a salad dressing, called vinegar.

You will see the structures of theacrine and caffeine below in Figure 2. Look closely at the right side of the molecules…theacrine has an oxygen atom and a methyl group (-CH3) that caffeine does not. Overall, they are extremely similar! The good news is that our bodies handle both of these comparably, but with a couple of modifications. And, in my opinion, favorably for theacrine.

theacrine-caffeine
Figure 2:
Chemical structures of theacrine and caffeine.

Due to the structural similarities between the two as purine alkaloids, thearcine and caffeine perform their duties in a very similar fashion in the body. Methylxanthines such as caffeine, theobromine, and theophylline have been found to act on adenosine receptors in the body (1). Theacrine does this as well, however, it is done through different binding actions. In addition, theacrine has also been hypothesized to alter the function of dopamine receptors in the brain along with influencing various neurotransmitters (e.g. GABA, acetylcholine) (2). These separate modes of action may help explain many of the additional benefits of theacrine when compared to caffeine.

How Good Is It?

Theacrine is found naturally in the Amazonian plant Cupuaçu as well as in the storied Chinese tea kucha (3). Kucha also contains moderate amounts of caffeine, from which theacrine is synthesized (4).

Unfortunately, theacrine doesn’t have piles of scientific papers examining its effect on the human body. However, there is one heavily cited paper from 2012 that has been used as the prime supporter of theacrine supplementation in human subjects (4). Feduccia et al. showed that, like caffeine, theacrine has a dose dependent effect (i.e. the more you take, the stronger the effects). But what are the effects?

  • Increased locomotion (activity)
  • Increased libido
  • Increased motivation
  • Increased mental acuity (concentration)
  • Increased pain tolerance
  • Decreased inflammation
  • Decreased fatigue
  • Decreased anxiety

That’s a pretty stellar list of attributes if you ask me! While the effects of theacrine begin to arise with only 50 mg, a majority of research studies used a relatively moderate dose of 200 mg of theacrine (seem familiar?) (2).

Of course, the degree of these effects will be dose and person dependent, but Habowski et al. demonstrated that these effects all reached peak levels roughly 4 hours after supplementation (2, Figure 3). You probably don’t want to take your preworkout 4 hours beforehand though. They also showed that about 80% of the peak effects were exhibited merely 1 hour after supplementation. Now that fits much better into your preworkout protocol!

theacrine-charts
Figure 3:
Efficacy of Theacrine VS Time (adapted from Reference 2).

Many of the effects of theacrine are the same as caffeine, so why not just dose up with caffeine, like we’ve been doing for ages? Because we become desensitized to caffeine over time. We’ve all experienced this. We up the dose, again, and again, then eventually nothing happens.

This doesn’t happen with theacrine. In fact, over a 7-day period, theacrine sensitization has actually been shown to INCREASE (4) and demonstrated that a single, daily dose of 300 mg TeaCrine® displayed no habituation over a full 8-week, comprehensive study (5). That means that we can either use the same dose and get better effects or decrease the dose and get the same results, whichever floats your boat. A few other advantages of theacrine when compared to caffeine are its anti-anxiety and anti-inflammatory effects (2,6-9). If you’d like you can even double up with theacrine (TeaCrine®) and caffeine to give yourself a longer lasting, yet smoother acting stimulatory ride.

As I alluded to earlier, the dosage of theacrine is similar to caffeine, but as with any supplement it is best to determine your own tolerance by starting slow. Many reports, both evidence-based and anecdotal, state that positive effects begin around 50 mg.

Dosages

Again, like any supplement (or substance), there is always an upper limit to supplementation. The LD50 (dose to kill half the population) of theacrine in mice is a high 750-850 mg/kg/day (caffeine weighs in at 127 mg/kd/day). That’s the equivalent of a 200 pound person sucking down 68-77 grams of theacrine (5). Needless to say, this would be quite difficult to accomplish, especially by accident.

The Real Deal?

When we get caffeine, we’re generally aren’t worried if it’s real, fake, or something else entirely. However, even protein powders have been faked in recent years. This is already been shown to be true with some sources of theacrine. So how can we know that we have theacrine and not caffeine, or creatine, or glucose powder? Honestly….we can’t. That is unless you have your own multimillion dollar testing lab. I

If we assume that what we’re told is in the bottle is actually in the bottle, then we can be sure that it is high quality, thanks to patents and trademarks. Many supplements nowadays are either patented and/or trademarked to ensure a higher quality product. You’ve almost certainly experienced this….CarnoSyn (beta-alanine), CreaPure (creatine monohydrate), HydroMax (glycerol). Theacrine has a high quality, trademarked version as well! TeaCrine® by Ortho-Nutra, LLC (patent link below article), distributed exclusively by Compound Solutions, Inc. What truly distinguishes TeaCrine® from generic theacrine is it is the only theacrine with a secured, supply chain of impeccable quality, reliability, purity and potency, informed-choice/sport, developed from a validated reference standard and assay method. TeaCrine® is also the first and only theacrine with multiple human clinical research studies & multiple global patents pending.

And you’d be remiss to believe that any product put out by the Mountain Dog doesn’t have the best of the best in it. This is exactly why products formulated by John contain TeaCrine along with HydroMax. Like John’s impeccable reputation, the supplements in his formulations carry a similar credibility.


AldenRynoAbout the author:

Alden is a lifestyle wellness coach, certified strength & conditioning coach, accredited nutritionist, avid bodybuilder, and eternal dog lover. At 20, he graduated from North Georgia College & State University in 2012 with a Bachelor’s in Chemistry. After which, he attended the Georgia Institute of Technology as a graduate student, but left upon completion of his PhD coursework in order to pursue his passion of educating and helping others attain healthier lives. After a year of personal training during 2014-15, he received the CPPS accreditation from Joe DeFranco and James “Smitty” Smith, then move to Las Vegas in July of 2015 to begin anew!

He’d love to hear from you concerning this article or anything else at algryno@gmail.com

Blog: xfitgen.com

Twitter: @alderslodge

Instagram: @alden_ryno


Patent Link:

https://www.google.com/patents/US20150132280


References:

  1. Synder, S., et al., “Adenoside receptiors and behavioral actions of methylxanthines.” Proc Natl Acad Sci U S A. 1981 May;78(5):3260-4. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC319541/
  2. Habowski, S. M., et al. “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.” Journal of the International Society of Sports Nutrition11.Suppl 1 (2014): Page 49. http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4271659/pdf/1550-2783-11-S1-P49.pdf
  3. Zheng, XQ; Ye, CX; Kato, M; Crozier, A; Ashihara, H (2002). “Theacrine (1,3,7,9-tetramethyluric acid) synthesis in leaves of a Chinese tea, kucha (Camellia assamica var. Kucha)”. Phytochemistry 60 (2): 129–34.doi:10.1016/s0031-9422(02)00086-9. PMID 12009315. http://www.sciencedirect.com/science/article/pii/S0031942202000869
  4. Feduccia, Allison A.; Wang, Yuanyuan; Simms, Jeffrey A.; Yi, Henry Y.; Li, Rui; Bjeldanes, Leonard; Ye, Chuangxing; Bartlett, Selena E. (2012). “Locomotor activation by theacrine, a purine alkaloid structurally similar to caffeine: Involvement of adenosine and dopamine receptors”. Pharmacology Biochemistry and Behavior 102 (2): 241. doi:10.1016/j.pbb.2012.04.014. http://www.sciencedirect.com/science/article/pii/S0091305712001244
  5. Hayward, S., et al., “SAFETY OF TEACRINE®, A NON-HABITUATING, NATURALLY-OCCURRING PURINE ALKALOID OVER EIGHT WEEKS OF CONTINUOUS USE” ISSN Poster Presentation, 2015
  6. Wang, Y., et al. “Theacrine, a Purine Alkaloid with Anti-inflammatory and Analgesic Activities.” National Center for Biotechnology Information. Fitoterapia, Sept. 2010. http://www.ncbi.nlm.nih.gov/pubmed/20227468
  7. Xie, Guo, et al. “Experimental Study of Theacrine on Antidepressant Effects.” Chinese Pharmacological Bulletin., Sept. 2009. http://en.cnki.com.cn/Article_en/CJFDTOTAL-YAOL200909013.htm
  8. Li, WX, et al. “Theacrine, a Purine Alkaloid Obtained from Camellia Assamica Var. Kucha, Attenuates Restraint Stress-provoked Liver Damage in Mice.” National Center for Biotechnology Information. J Agric Food Chem, July 2013. http://www.ncbi.nlm.nih.gov/pubmed/23678853 http://goo.gl/5H3ErV
  9. Li, Y., et al. “Theacrine, a purine alkaloid derived from Camellia assamicavar. kucha, ameliorates impairments in learning and memory caused by restraint-induced central fatigue.” J. of Func.Foods, 16, June 2015, Pages 472-483. http://www.ncbi.nlm.nih.gov/pubmed/23678853