As someone just like you that is looking for a safe, effective and legal edge to help improve body composition, health and quality of life, I take great pride in introducing what Agmatine is, where it comes from, what it can do and more.

By: Joey Rodrigues & Dr. Dana Houser, MD, MHSA


Introduction

Today I sit here with excitement about a ground-breaking nutrient that I have the pleasure to introduce to the sports nutrition world.

Before I begin discussion about what this new ground breaking nutrient (Agmatine) is and what it means to you, the active lifestyle enthusiast, let me make some things perfectly clear to you right here and right now.

As someone just like you that is looking for a safe, effective and legal edge to help me improve my body composition, health and quality of life, I take great pride in running a company that is committed to introducing innovative and result-driven concepts that are supported by science.

I know you have heard that type of jibba jabba before from every supplement company representative under the sun, but I am speaking the truth and those of you who are familiar with my company and concepts know this man!

I also want to let you know that I am simply an individual with a voice that serves as a bridge for you today to information that can lead to improved body composition, health and performance. While this introduction today is very exciting, and very real, I cannot take credit for its invention as is the practice by many Supplement Companies and owners today.

You see, I did not invent nor discover Agmatine, but I do want to be the man that helps educate you on this truly miraculous nutrient. There are real scientists out there that actually discover these grand innovations, and other pioneers in our industry such as the late great Dan Duchaine, Dr. Dan Gwartney and even Thomas Inclendon that have an intricate knowledge of biochemistry and how this impacts real-life applications.

In fact, all these great men have spoken of Agmatine several years ago. But, it was an article written by Dr. Dan Gwartney some 8 years ago that peaked my interest about this ever-so-versatile byproduct of the amino acid Arginine.

What I will take credit for is making it a reality to you the people and again as a source of information that may contribute to your growth.

At the risk of sounding like Bill Phillips when he compared the branched chain amino acid, Leucine-metabolite, HMB (B-hydroxy B-methylbutyrate) to the anabolic steroid known as Deca, I am putting my name and street cred on the line by dubbing Agmatine "The Holy Grail of Supplements". You read correctly and as we get further along into this discussion you may even realize that I'm not that crazy after all.

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Agmatine
Fascination Of An Industry With A Molecule That Holds More Promise Than Arginine

As mentioned above, Agmatine ((4-aminobutyl) guanidine, NH2-CH2-CH2-CH2-CH2-NH-C(-NH2)(=NH )) is a byproduct of Arginine that is produced through a process called decarboxylation. It is basically Arginine with the carboxylic acid end removed.

Nearly anyone hip to the supplement game is up on Arginine. Many years back, Arginine was heavily promoted by Life Extensionists (most notably, Shaw and Pearson) and sports nutritionists (Dr. Michael Colgan) as a big GH releaser. It has most recently regained popularity as one of the hottest supplements in sports nutrition for its role in the production of Nitric Oxide (NO).

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Just walk into any sports nutrition store and look at any supplement line and you are bound to see a host of NO products. Supplement companies are pumping Arginine pills out faster than McDonald's is slanging Happy Meals to toddlers. "Skin bursting pumps," "enhanced nutrient delivery" and "sheer SIZE" are attributes being heavily touted as a result of Arginine supplementation in various forms. See, Ethyl Ester Mania!

Arginine does have many benefits to both the bodybuilder as well as person seeking general health improvement. Arginine is well documented for its ability to support endogenous production of creatine, stimulation of protein synthesis, insulin sensitivity through attenuation of blood glucose, GH production, and its role in the urea cycle to aid in the removal of nitrogenous waste.

It may even have a general health role for those that have suffered from heart failure and/or a heart attack, as well as a potential aid in sexual dysfunction cases, including enhancement of spermatogenesis (sperm production), either as a standalone or in conjunction with synergistic nutrients via its vasodilatory properties. Arginine's effects truly seem to be unsurpassed.

That is, until now! Agmatine is likely the one molecule to take part in more metabolic processing than Arginine. There are nineteen well-accepted mechanisms of action suggested in the literature and at least thirteen have direct benefits to the bodybuilder and/or health enthusiast with even more effects being discovered literally on a daily basis!


Locating Agmatine

In the body, Agmatine is widely and unevenly distributed. It has been identified in the stomach, aorta, small intestine, large intestine, spleen, lung, vas deferens (of the male genital tract), adrenal gland, kidney, heart, liver, skeletal muscle, the testes, and brain. The concentration of agmatine varies in different parts of these organs.

The highest concentrations of which were the stomach, aorta, and small intestine. However, since the enzyme that converts Arginine into Agmatine has not been confirmed in the fundus of the stomach and/or intestine, it has been debated by some that either an independent source of agmatine also exists or that it should be obtained through bacterial colonization or the diet, and absorbed via a specific transporter.

Anatomy Video.
Click Play To Start The Video.

All foods are made up of hundreds of naturally occurring compounds that can have varying effects on us, depending on how much we eat and how sensitive we are. Biogenic amines - like Agmatine - are formed by the breakdown of proteins in foods. Foods like beef, fish, bananas, avocados, mushrooms, chocolate, sauerkraut, and soy sauce are just some that contain Agmatine to varying degrees, though these levels can vary precipitously and drastically alter the amount you are ingesting.

The problem is that as we age, it appears that our levels of amines decline. This can have disastrous effects on mental functioning, blood pressure, body temperature, amongst many others we will discuss momentarily.

Did You Say Holy Grail?

    Yes we did. And here's why. The effects of this highly versatile nutrient can be divided into two groups based on the individuals that choose to use it. The athlete or life extensionist, both of which continue to strive for the healthy lifestyle, can expect different effects from agmatine to aid in attaining their goals. The benefits here are not mutually exclusive and therefore you may see the same effects listed for both camps.


Agmatine & The Athlete

  1. Agmatine is a pain fighter. This can be beneficial to the athlete in two ways:
    1. It can potentiate the effects of analgesics used during recuperation from injury.
    2. It has the potential to aid post-workout recovery.
  2. Agmatine enhances insulin production leading to better insulin response. This allows for positive effects in attaining body composition goals. Better insulin response means a harder and leaner more muscular body.
  3. Agmatine acts on various hypothalamic and pituitary peptide hormones such as LH and GH. These will have subsequent effects on other hormones like IGF-1. Control of the hormonal environment of the athlete and you will perform better, look better and feel better.
  4. Agmatine possesses anxiolytic (relieves anxiety) and antidepressant properties offering potential control of cortisol levels in the stressful life of the athlete.
  5. Agmatine modulates nitric oxide (NO) through different ways. It stimulates some types of nitric oxide synthase (NOS) while inhibiting others. This is essential to the proper functioning of the polyamine biosynthetic pathways.
  6. Agmatine acts on catecholamine (Epinephrine > Norepinephrine > Dopamine) release. These endogenous compounds are part of nearly every action in the body. Most notably for the athlete is the role that this compound would ultimately have in both energy production and aiding anticipation of the stress afforded by competition. However, there are also well-established roles that epinephrine can have on the body that includes:

  7. Agmatine has an antioxidant role. There can be no greater source of free-radical build up than that seen in the day-to-day activity of the athlete. The sheer stress that the body takes on when in you're an athlete in the trenches (i.e. - the gym, the field, etc...) could ultimately have significant detrimental effects with continued build up. Agmatine can offer protection from the undesired effects that free radicals can have on the body.
  8. For the athlete desiring body composition change, Agmatine has an independent role of insulin and testosterone management on lipid (fat) metabolism.

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  1. Agmatine possesses nootropic effects (it acts as a "novel" neurotransmitter). This can offer the athlete a potential mental edge to prepare for various events.
  2. Agmatine can aid in kidney function by stimulating the glomerular filtration rate (GFR). This can bode the bodybuilder well as various nitrogenous waste products are removed through this system.
  3. Agmatine harbors a hypotensive role which could assist the exogenously-enhanced athlete in keeping blood pressure in check.


Agmatine & The Life Extensionist

  1. Agmatine has a neuroprotective role. The life extensionist will likely see this as a positive effect in cases of such chronic diseases as Alzheimer's Dementia. This is thought to originate through a couple of mechanisms, but most notably its prevention of over-excitation by glutamate and its antioxidant roles.
  2. Agmatine can assist in chronic pain management. Sufferers of things such as chronic degenerative diseases that do not get adequate relief from various pharmaceutical analgesic agents may see agmatine as the ideal adjunct to their current treatment.
  3. Pain
    Click Image To Enlarge.
    Agmatine Can Assist In Chronic Pain Management.

  4. Agmatine's antioxidant role has significant impact on one of the unifying themes of aging in oxidative stress accumulation and its contribution to the aging individual.
  5. Agmatine may possess a role in cancer prevention via its modulation of all polyamine biosynthetic pathways. This effect may be limited to vascular growths via smooth muscle cell overgrowth. Control of cell growth can be attributed to two different pathways:
    1. A membrane receptor controlled pathway
    2. A pathway dependent on cellular polyamine content
  6. As mentioned earlier, agmatine imparts action on various hypothalamic and pituitary peptide hormones such as LH and GH. Control of the hormonal environment of the anti-aging medicine enthusiast can point rather quickly at the positive effects this can have.
  7. Agmatine can aid in kidney function by stimulating the glomerular filtration rate (GFR) which can positively impact those suffering from chronic kidney diseases.
  8. Agmatine enhances insulin production leading to better insulin response. As we grow older this impacts glycation. Glycation is the process where sugars attach to blood proteins and results in a complex series of rearrangements and oxidative reactions leading to advanced glycation end-products (AGEs).

    It is this complex series of events that agmatine hits at its core and could prove synergistic with other molecules (i.e. - carnosine) in our fight to remain young.

  9. Agmatine's hypotensive role has implications here as our continued assurance of fending off the cardiovascular sequelae that offer the deleterious effects of metabolic derangements such as the virtually epidemic diabetes and obesity run rampant.
  10. Diabetes:

    Obesity:


The Bottom Line

Even our most devout supporters thought we were off our rocker when we were so bold as to anoint Agmatine as the "Holy Grail of Supplements". And rightfully so. It is the sad truth that as a consumer (we include ourselves in this list) that you have been burned more often than not by supplement companies and their grand innovations.

The likes of smilax, boron, chromium picolinate, all-in-one products, as well as far too many others to list have left you snubbed and short on coin. This brief introductory article into the Who, What, When, Where and Why of Agmatine should serve at the very least as some merit to our claims and interest in a fascinating new nutrient that may even make Arginine supplementation obsolete.

In part two, Dana Houser MD, MHSA (dinoiii), Shawn D. Wells MPH, RD (Androgenic) and Joey Rodrigues CEO/Founder will take part in a round table discussion that will take a deeper look into Agmatine. We will elaborate on mechanisms of actions/effects and what that means to you.

We will also provide real world feedback from our own personal experiences using Agmatine and provide recommendations on how to implement its use on a daily basis along with what supplements/products can be used in conjunction with Agmatine. Until then, we wish you the best in your quest for improved body composition, health and quality of life.

References:

  1. Abe K, Abe Y, and Saito H. Agmatine suppresses nitric oxide production in microglia. Brain Res. 872: 141-148, 2000.
  2. Aricioglu-Kartal F, and Regunathan S. Effect of chronic morphine treatment on the biosynthesis of agmatine in rat brain and other tissues. Life Sci. 71: 1695-1701, 2002.
  3. Gao, Y., et al. Agmatine: a novel vasodilator substance. Life Sciences. 57(8):PL83-86, 1995.
  4. Halaris A, Piletz JE. Imidazoline receptors: possible involvement in the pathophysiology and treatment of depression. Hum Psychopharmacol. 16(1):65-69, 2001.
  5. Kalra, S.P., et al. Agmatine, a novel hypothalamic amine, stimulates pituitary luteinizing hormone release in vivo and hypothalamic luteinizing hormone-releasing in vivo. Neuroscience Letters. 194 (3): July 21, 1995; 165-168.
  6. Kawabata T, Ohshima H, Ino M. Occurrence of methylguanidine and agmatine in foods. IARC Sci Publ. (19):415-23, 1978.
  7. Lortie, M.J., et al. Agmatine, a bioactive metabolite of arginine. Production, degradation, and functional effects in the kidney of the rat. Journal of Clinical Investigation. 97(2):413-420, 1996.
  8. Morgan, N.G., et al. Characterization of the imidazoline binding site in regulation of insulin secretion. Annals of the New York Academy of Sciences. 763:361-373, 1995.
  9. Nishimura K, Shiina R, Kashiwagi K, and Igarashi K. Decrease in Polyamines with Aging and Their Ingestion from Food and Drink. J of Biochem. 139(1):81-90, 2006.
  10. Raasch, W. et al. Agmatine, the bacterial amine is widely distributed in mammalian tissues. Life Sciences. 56(26):2319-2330, 1995.
  11. Raghavan SA, Dikshit M. Vascular regulation by the L-arginine metabolites, nitric oxide and agmatine. Pharmacol Res. 49(5):397-414. Review, 2004.
  12. Regunathan S, Feinstein DL, and Reis DJ. Anti-proliferative and anti-inflammatory actions of imidazoline agents. Are imidazoline receptors involved? Ann NY Acad Sci. 881: 410-419, 1999.
  13. Regunathan S, and Reis DJ. Characteristics of arginine decarboxylase in rat brain and liver: distinction from ornithine decarboxylase. J Neurochem. 74: 2201-2208, 2000.
  14. Reis DJ, and Regunathan S. Agmatine a novel neurotransmitter? Advances in Pharmacology. 42:645-649, 1998.
  15. Schwartz D, Peterson OW, Mendonca M, Satriano J, Lortie M, and Blantz RC. Agmatine effects glomerular filtration rate via a nitric oxide synthase-dependent mechanism. Am J Renal Physiol. 272: F597-F601, 1997.
  16. Sener A, et al. Stimulus-secretion coupling of arginine-induced insulin release. Insulinotropic action of agmatine. Biochemical Pharmacology. January 15, 1989. 38(2):327-330, 1989.
  17. Tabor CW, and Tabor H. Polyamines. Ann Rev Biochem. 53: 749-790, 1984.
  18. Vargiu C, Cabella C, Belliardo S, Cravanzola C, Grillo MA and Colombatto S. Agmatine modulates polyamine content in hepatocytes by inducing spermidine/spermine acetyltransferase. Eur. J Biochem. 259: 933-938, 1999.
  19. Weitzel G., et al. Insulin-like partial effects of agmatine derivatives in adipocytes. Hoppe-Seylers Zeitschrift fur Physiologische Chemie. 361(1):51-60, 1980.
  20. Yananli H, Goren MZ, Berkman K, Aricioglu F. Effect of agmatine on brain l-citrulline production during morphine withdrawal in rats: A microdialysis study in nucleus accumbens. Brain Res. 2007 Feb 9;1132(1):51-58, 2006.
  21. Zarandi M, Serfozo P, Zsigo J, Deutch AH, Janaky T, Olsen DB, Bajusz S, Schally AV. Potent agonists of growth hormone-releasing hormone. II. Pept Res. 5(4):190-3, 1992.

Joey Rodrigues & Dr. Dana Houser, MD, MHSA

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BigDaddyFlea

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Good article, thorough and academic. Definitely going to give this a shot

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pcp135

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This is a lazily written article that either assumes readers are experts who know the references by heart or will be placated by the list at the end.

"Arginine does have many benefits to both the bodybuilder as well as person seeking general health improvement. Arginine is well documented for its ability to support endogenous production of creatine, stimulation of protein synthesis, insulin sensitivity through attenuation of blood glucose, GH production, and its role in the urea cycle to aid in the removal of nitrogenous waste."

The quoted paragraph above should have reference after each of the claims at the end. I am surprised this is written by MDs. I have never read an article with this type of referencing style. It basically leaves you to either do a lot of work to chase down all the reference and associate them with each claim or take the writers' credentials as being enough to believe the claims.

May 30, 2014 9:48am | report
 
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