AICAR
(5-Aminoimidazole-4-carboxamide ribonucleoside), also known as Acadesine, is a metabolic modulator and an analog of adenosine. It is widely used in scientific research as an “exercise mimetic” due to its ability to stimulate pathways typically activated by physical activity.
1. Biological Function and Mechanism
- AMPK Activation: Once inside a cell, AICAR is converted into ZMP (AICA ribotide), which mimics AMP (adenosine monophosphate). This activates the AMP-activated protein kinase (AMPK), a master regulator of cellular energy homeostasis.
- Energy Regulation: When AMPK is activated, it shifts the cell’s metabolism from anabolic processes (building molecules) to catabolic processes (breaking down molecules for energy).
- Mitochondrial Biogenesis: Research indicates that AICAR can trigger cells to produce more mitochondria, increasing the efficiency of energy creation.
2. Potential Therapeutic Uses
Ongoing research in 2026 explores AICAR’s potential for various conditions:
- Metabolic Disorders: It has shown promise in animal studies for treating Type 2 Diabetes and metabolic syndrome by improving insulin sensitivity and reducing fatty acid synthesis.
- Cardioprotection: It was historically investigated for its ability to reduce cardiac injury by increasing adenosine levels during periods of low blood flow.
- Neuroprotection: Studies suggest it may have anti-inflammatory effects in the brain and could potentially treat neurodegenerative diseases.
3. Use in Sports and Doping
AICAR is famously known as an “exercise pill” because it can enhance endurance without physical exertion.
- WADA Status: As of 2026, AICAR remains on the World Anti-Doping Agency (WADA) prohibited list under the category of “Hormone and Metabolic Modulators”.
- Performance Enhancement: It is banned because it increases fat oxidation and improves endurance performance, providing an unfair advantage to athletes.
4. Chemical and Storage Properties
- Chemical Formula:
C9H14N4O5cap C sub 9 cap H sub 14 cap N sub 4 cap O sub 5
𝐶9𝐻14𝑁4𝑂5
.
- Appearance: Typically a white crystalline solid.
- Storage: For research purposes, it is generally stored at -20°C to maintain stability.
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