Too much activation of AMPK, or activating it in the wrong tissue, can cause serious side effects, including neurodegeneration, or preventing cells from dividing.
#AMPK ACTIVATOR ACTIVATOR#
Some articles refer to AMPK activators as “exercise-in-a-pill” in the hope that using an AMPK activator will cause the same changes in the body as exercise. Why is AICAR on the World Anti-Doping Agency (WADA) Prohibited List?ĪICAR is prohibited because it’s an AMPK activator, which are prohibited at all times under the category of Hormone and Metabolic Modulators on the WADA Prohibited List because of their potential performance-enhancing effects. To date, the medical community has not found a way to target AMPK in a way that allows for the treatment of diseases in humans, although research has suggested it plays a role in diabetes, heart disease, and cancer. The effects of activating AMPK are extremely complex since it is involved in so many different metabolic pathways of the body. There are many circumstances that activate AMPK naturally, including hypoxia (low oxygen levels during exercise or at elevation), hypoglycemia (low blood sugar with exercise or fasting), the use of cellular energy during muscle contraction, and anything that disrupts energy creation within cells. AMPK basically ensures that the various tissues in the body don’t run out of energy. For example, it increases the usage of fat for energy and causes cells to make more mitochondria (the cells’ powerhouses or energy creators). Once activated by AICAR, AMPK works to make energy more available. How do AICAR and AMPK impact performance? The AMPK-stimulating AICAR can also be synthesized in a lab and is being evaluated in preclinical research and human clinical trials as a therapeutic agent to treat certain metabolic disorders in humans.
AMPK acts as an energy regulator and is activated during exercise or other circumstances that use up cellular energy.
What is AICAR?ĪICAR (5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside) is a substance produced naturally by the body that stimulates AMP activated protein kinase (AMPK), a protein that regulates metabolism in a variety of ways. Here’s what athletes should know about AICAR and other prohibited AMP activated protein kinase activators. However, this substance is both prohibited in sport and a health risk because it’s not approved for therapeutic use in humans anywhere in the world. In recent years, AICAR has been in the news a number of times as a novel substance athletes have turned to for performance enhancement.