AICAR (5-Aminoimidazole-4-carboxamide ribonucleotide) How Does It Work?

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AICAR, or 5-Aminoimidazole-4-carboxamide ribonucleotide for those who like specifics, is a substance that has actually been around for almost two decades now. Recently it has come back into the limelight. It's primary role for people like us is as an endurance enhancer. Yes, much like GW50 (in fact, they stack nicely together). And much like GW50, AICAR is not actually a SARM. GW50 is a PPAR-delta agonist and AICAR is a PPAR-delta AMPK axis agonist. Yeah, lets just say both are SARMs for sake of simplicity and move on. :) The beautiful part about AICAR is that your body already naturally makes some of this enzyme, making it harder to detect those who dope with it. The Anti-Doping people have tested some of the best athletes in existence and used their scores as a "limit" to see if someone is doping with AICAR. If you are significantly over what the best athletes naturally have, odds are you are doping...or at least that is their going theory.


AICAR stimulates AMP-activated protein kinase (which is an enzyme) activation, which basically does a few things for us that we want to increase:
1. Stimulates the burning of Liver Fatty Acids (which is good for the liver)
2. Inhibits the creation of Cholesterol
3. Inhibits the creation of Fats (lipogenesis)
4. Stimulates the intake of glucose into muscles while reducing the body's use of insulin
5. Greatly aided in maintaining consistent glucose levels in diabetics


It certainly does many other things (such as aiding in the removal of leukemia cells), but those are the big ones most people will care about, with number 4 being the big one that increases endurance. More energy for your muscles means they can work longer without getting tuckered out and crying for you to stop.


It also aids in rushing blood to the cells of the heart, and has long been used by the medical community to perform what is called "heart preconditioning" prior to doing heart surgery or other surgeries where they have to stop the heart. It helps the heart recover from trauma much faster.


Now we get into some real numbers - how much DOES AICAR help you as an athlete and how much did they use in the studies? The study was of both GW50 and AICAR and as such I will include number for both, for comparison.


Treating mice with GW501516 (10 mg/kg/d) for 5 weeks in conjugation with physical training increased their performance time by approx. 70% compared to their non-drugged counterparts. Moreover, it was shown that GW501516 enhanced the influence of exercise on the whole body (5).

However, the results of studies with AICAR, the analogue of adenosine monophosphate, were far more striking. After 4 weeks of AICAR application (500 mg/kg/d) the sedentary mice were running by 23% faster and by 44% further than untreated and untrained mice (5). This report confirmed former studies that had shown that 5 days of AICAR treatment may lead to the increased levels of glycogen, glucose transporter GLUT4 and mitochondrial enzymes in mice (16).
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Hmmm....10mg/kg of GW50 and 500MG/KG of AICAR? No human would ever use those numbers. The recommended human doses for those who want an endurance boost is 20mg a day of GW50 and 25mg a day of AICAR. From what I can find, there are no studies showing the effects of such low levels. From my personal use, I have found that GW50 greatly increased my endurance, which a side effect that I no longer dreaded doing cardio. Cardio no longer made me feel like crap afterwards (which is why so many dread it). I doubled the time I spend in a single cardio session (from 20 mins to 40 mins) and still feel more alive afterwards than before I used GW50. I have yet to use AICAR, but plan to soon. I will replace my normal GW50 use with AICAR and see how it compares.


The only negative effect found due to AICAR use (so far, limited human studies have been done and no longer term studies at all) is the slow, but sure, increase in lactic acid in muscles. This is no surprise, since you are using the muscles longer and harder than you normally could so the build up would be higher than normal as well. Just remember to get good sleep after every day where you kill it in cardio to allow the muscles to recover.


One big difference between GW50 and AICAR is that GW50 requires exercise in order to do its magic while AICAR does not. Yes, you can sit on your ass watching Television and AICAR will still do its magic. Of course, exercising as well will give you much, much better results, but that explains why they are still testing AICAR as a viable drug for those who are incapable of getting the needed exercise (bed ridden, etc).


For me, AICAR sounds like a good thing and might very well be what they claim it to be - exercise in a bottle.



References:
https://www.researchgate.net/public...ulated_glucose_transport_in_3T3-L1_adipocytes
5-Aminoimidazole-4-carboxamide ribonucleoside treatment improves glucose homeostasis in insulin-resistant diabetic (ob/ob) mice. - PubMed - NCBI
Isoform-selective 5'-AMP-activated protein kinase-dependent preconditioning mechanisms to prevent postischemic leukocyte-endothelial cell adhesive ... - PubMed - NCBI
JPP No 4/2014 article 02
 
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