Ingredient Selection for NO3X
Since the increasing regulation of DMAA (1,3-dimethylamylamine), there has been a real push for many companies to find effective stimulant replacements, which are clearly stronger than caffeine yet are safe and legal.
Unfortunately, this has been a large hurdle and many companies have simply substituted by putting very large amounts of caffeine in their products, upwards of 400mg per serve, which when correctly labelled would render them illegal in Australia (where max doses per serve are restricted), and not particularly safe when undisclosed.
Over the last 12 months Bulk Nutrients has worked extensively in house and with our BioChemist, both on the research of literature and the physical blending of effective ingredients, particularly the use of MAO-B inhibitors to increase stimulant activity. In summary, these (MAO inhibitors) work by suppressing an enzyme in the body (Monoamine oxidase) which breaks down compounds and renders them inert.
Phenylethylamines (which there are many derivatives) are of particular interest here, as when MAO-B is suppressed effectively, various PEAs could form the basis of a very effective pre workout product. Basically, effective suppression of MAO-B equals an equally effective stimulant hit. The science here gets quite complicated, but it’s the reason why some substances are extremely effective stimulants and similarly structured phenylethlamines have virtually no impact on the body/brain, as they are metabolised almost instantly.
Much of this suggestion on MAO inhibition was based on solid theory, as well as the claims of “Crazed “and other U.S products, however while the marketing of these mentioned MAO inhibition, there was little to determine from their ingredient lists that any effective inhibitors were actually used – and we can assure you a lengthy analysis was done.
Interestingly, Bulk Nutrients submitted a sample of “Crazed” for mass spectrometry at a laboratory with curious results. Without giving too much away, based on what appeared to be present, we were not completely surprised when it was eventually taken off the market, and we don’t believe that effective inhibition of MAO-B played any significant role in the stimulant strength of this product.
The challenges with MAO inhibitors here were many, while various compounds could be found that were effective MAO inhibitors, many inhibited MAO-A which was a definite unwanted side effect, and of course many were listed pharmaceuticals! Inhibiting MAO-A can actually be dangerous, particularly for those taking anti-depressants.
Over a period of 6 months we trialed many versions of what appeared to be potent natural extracts, Psoralens and similar extracts for this purpose, with none giving significant advantages here. Much of the problem revolved around time of activation (which is difficult when all ingredients are taken at the same time as in a pre-workout), half-lives and cost.
Eventually some potentially very effective ingredients were discovered, however at a cost of several hundred dollars per gram, they were not even close to being commercially viable in any form. Once we had completed the long and very costly process of realising MAO inhibition using available ingredients would only play a minor effect, we focused our attention elsewhere.
Being close to the ground, we are always very aware of new compounds hitting the market, and International suppliers often offer all kinds of ingredients with much enthusiasm. From N Methyl Tyramine, Higenamine, Halostachine, and extracts like Arcacia Rigidula, Dendrobium and many more were all trialed with various results. None however, seemingly regardless of the combination used were significantly powerful, so none made the grade.
Eventually some testing was done with 2 amino 4 methylpentane which immediately looked positive due to its structure. 2 Amino 4 Methylpentane is often shortened to Amp Citrate, with the letters Amino Methyl Pentane forming a natural abbreviation. Amp Citrate has been used in the U.S for more than 6 months in commercial products, appearing in products such as Genomyx Evol, Ampitropin and Pre Amp.
Structurally, it has similarities to DMAA which is why these is no surprise that the effects are pronounced. It appears to provide the necessary stimulant effects, with increased alertness, focus and energy, with less unwanted side effects such as increased heart rates and most importantly works well with Caffeine and Hordenine (mild MAO-B inhibitor, alpha- and beta-adrenergic stimulant).
Given the ingredient has only had recent commercial use, we would advise any users to use caution when dosing and only consume a maximum of one dose of the product per day. Individuals who compete in ASADA tested events should take particular note here however as 2 amino 4 methylpentane was recently banned for in competition use.