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  • Erick A. Mosteller

AICAR: Navigating the Thin Line Between Athletic Enhancement and Health Risks


AICAR, a synthetic peptide touted for its potential benefits in treating metabolic disorders and enhancing exercise performance, presents a dichotomy that demands a critical evaluation. While its ability to mimic the effects of AMP and activate AMPK holds promise for various physiological improvements, the associated risks, particularly for athletes, cannot be overlooked.


The mechanism through which AICAR stimulates AMPK, a crucial regulator of cellular energy balance, is intriguing. By affecting glucose uptake, fatty acid metabolism, mitochondrial function, and muscle endurance, AICAR demonstrates a multifaceted potential to address metabolic issues and boost physical performance. However, the perilous aspect lies in its unapproved status for human use, rendering it a prohibited substance in sports and raising concerns about unknown long-term effects.


What are the potential benefits of AICAR?


AICAR has been shown to have several potential benefits for treating metabolic disorders and enhancing exercise performance in animal models and human trials. Some of these benefits are:

  • AICAR can improve glucose uptake and utilization by skeletal muscle and reduce blood glucose levels, which can be beneficial for patients with type 2 diabetes or insulin resistance. AICAR can also increase the expression and activity of glucose transporter 4 (GLUT4), which is responsible for transporting glucose into muscle cells. AICAR can also enhance the sensitivity and signaling of insulin, which is the hormone that regulates glucose metabolism.

  • AICAR can increase the oxidation and breakdown of fatty acids by activating enzymes such as carnitine palmitoyltransferase 1 (CPT1) and acetyl-CoA carboxylase (ACC), which are involved in fatty acid transport and synthesis, respectively. AICAR can also reduce the accumulation and storage of lipids in adipose tissue and liver, which can prevent or reverse obesity, fatty liver disease, and dyslipidemia.

  • AICAR can increase the production and function of mitochondria, which are the organelles that generate energy for the cells. AICAR can also increase the expression and activity of proteins that are involved in mitochondrial biogenesis, such as peroxisome proliferator-activated receptor gamma coactivator 1-alpha (PGC-1α), nuclear respiratory factor 1 (NRF1), and mitochondrial transcription factor A (TFAM). AICAR can also enhance the efficiency and quality of mitochondrial respiration, which can improve the cellular energy status and prevent oxidative stress and damage.

  • AICAR can increase the endurance and performance of skeletal muscle by increasing the proportion and activity of slow-twitch fibers, which are more resistant to fatigue and rely more on oxidative metabolism. AICAR can also increase the blood flow and oxygen delivery to the muscle by stimulating the production of nitric oxide (NO) and vascular endothelial growth factor (VEGF), which are molecules that regulate vasodilation and angiogenesis, respectively. AICAR can also reduce the accumulation of lactate and hydrogen ions, which are byproducts of anaerobic metabolism that cause muscle fatigue and pain.

  • AICAR can protect the heart and blood vessels from ischemic injury, which is caused by a lack of oxygen and nutrients due to a blockage or narrowing of the arteries. AICAR can increase the tolerance and recovery of the cardiac tissue from ischemia and reperfusion, which is the restoration of blood flow after a period of ischemia. AICAR can also reduce the inflammation and oxidative stress that are associated with ischemic injury, by inhibiting the activation of nuclear factor kappa B (NF-κB) and the production of reactive oxygen species (ROS), which are molecules that trigger inflammatory and oxidative responses.


What are the potential risks of AICAR?


AICAR is a prohibited substance in sport and a health risk for athletes, as it is not approved for human use and has unknown long-term effects. Some of the potential risks are:

  • AICAR can cause adverse effects on the liver and kidney, which are the organs that are responsible for the metabolism and excretion of AICAR and its metabolites. AICAR can increase the levels of liver enzymes, such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST), which are indicators of liver damage. AICAR can also increase the levels of creatinine and blood urea nitrogen (BUN), which are indicators of kidney dysfunction.

  • AICAR can cause adverse effects on the brain and nervous system, which are sensitive to changes in the levels of nucleotides and energy status. AICAR can alter the levels of neurotransmitters, such as dopamine, serotonin, and acetylcholine, which are molecules that regulate mood, cognition, and behavior. AICAR can also affect the levels of neurotrophic factors, such as brain-derived neurotrophic factor (BDNF) and nerve growth factor (NGF), which are molecules that support the survival and growth of neurons. AICAR can also induce neurodegeneration, which is the loss of neurons and their connections, by activating the enzyme poly(ADP-ribose) polymerase (PARP), which is involved in DNA repair and cell death.

  • AICAR can cause adverse effects on the immune system, which is involved in the defense and regulation of the body against pathogens and diseases. AICAR can modulate the activity and function of various immune cells, such as macrophages, T cells, and B cells, which can have either beneficial or detrimental effects depending on the context and the balance of the immune response. AICAR can also affect the levels of cytokines, such as interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α), which are molecules that mediate inflammation and immunity.

  • AICAR can cause adverse effects on the reproductive system, which is involved in the production and regulation of sex hormones and gametes. AICAR can alter the levels of gonadotropins, such as luteinizing hormone (LH) and follicle-stimulating hormone (FSH), which are hormones that stimulate the production and maturation of sperm and eggs. AICAR can also affect the levels of sex steroids, such as testosterone and estrogen, which are hormones that regulate the development and function of the male and female reproductive organs and characteristics.


In conclusion, while AICAR holds promise as a therapeutic agent, its unregulated status and potential health risks, particularly for athletes, cast a shadow over its viability. The benefits in metabolic improvement and exercise performance must be weighed against the considerable risks, spanning multiple physiological systems. Until comprehensive research addresses the long-term effects and safety profile of AICAR, its use by athletes or individuals without proper medical supervision remains unwarranted. AICAR's journey from a naturally occurring peptide to a synthetic compound raises critical questions about the ethical implications of its unregulated use in pursuit of athletic excellence.





Erick Mosteller is a 35 year entrepreneur and business development consultant who is passionate about elevating critical understanding through effective information. Mr. Mosteller has degrees in ethnography, business administration, and International Marketing. Mosteller believes development of the rational mind and thoughtful training of the reactive mind is the key to long lasting happiness and understanding. Stay tuned for greater insights.

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Ayan Khan
Ayan Khan
Dec 02, 2023
Rated 5 out of 5 stars.

nice one

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