AICAR Peptide: What It Is, How It Works and the Research
AICAR peptide is 5-aminoimidazole-4-carboxamide ribonucleoside, a small molecule that switches on the energy enzyme AMPK. Despite the name, it is not a peptide. In people, its measured effects are small, and it is on the World Anti-Doping Agency (WADA) Prohibited List.
Sources: Human study. Cuthbertson DJ et al. 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men. Diabetes, August 2007. PMID 17513706. Supports: short-term muscle glucose uptake in people; Animal study (mice). Tukhovskaya EA et al. AICAR Improves Outcomes of Metabolic Syndrome and Type 2 Diabetes Induced by High-Fat Diet in C57Bl/6 Male Mice. International Journal of Molecular Sciences, 11 December 2022. PMID 36555360. Supports: full name of AICAR, AMPK activator, body weight and liver findings in mice; Lab method study (anti-doping). Buisson C et al. Implementation of AICAR analysis by GC-C-IRMS for anti-doping purposes. Drug Testing and Analysis, November 2017. PMID 29032594. Supports: naturally occurring, on the WADA Prohibited List, claimed performance effect
Short answer
- What is AICAR?
- A ribonucleoside the body makes naturally. As a drug it was called acadesine.
- What does it do?
- It turns on AMPK, the cell's energy sensor.
- Does it work in people?
- Only weakly so far. A short boost in muscle sugar uptake, and no direct effect on sugar uptake in a drip study.
- Is it allowed in sport?
- No. WADA prohibits it, and labs test urine for it.
Sources: Human study. Cuthbertson DJ et al. 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men. Diabetes, August 2007. PMID 17513706. Supports: short-term muscle glucose uptake in people; Human study. Bosselaar M et al. Intravenous AICAR during hyperinsulinemia induces systemic hemodynamic changes but has no local metabolic effect. Journal of Clinical Pharmacology, October 2011. PMID 21148051. Supports: heart rate, blood pressure, conversion to ZMP; Lab method study (anti-doping). Polet M et al. Rapid Analysis of Urinary AICAR by Liquid Chromatography-Isotope Ratio Mass Spectrometry. Analytical Chemistry, 21 April 2026. PMID 41955491. Supports: prohibited in sports under WADA rules; Drug profile (review). Acadesine: AICA riboside, ARA 100, arasine, GP 1 110. Drugs in R&D, 2008. PMID 18457469. Supports: other names; development for ischaemia-reperfusion injury and chronic lymphocytic leukaemia; Review. Drew BG et al. Acadesine, an adenosine-regulating agent with the potential for widespread indications. Expert Opinion on Pharmacotherapy, August 2008. PMID 18671468. Supports: adenosine and AMPK effects, poor oral bioavailability
What AICAR Is, and Why It Is Not a Peptide
AICAR is a ribonucleoside. Its full name shows that. A ribonucleoside is built on a ribose sugar. A peptide is a chain of amino acids. AICAR has no amino acid chain, so the word peptide does not fit.
It has other names too. Anti-doping papers write it as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside. As a drug it was AICA riboside, or acadesine. It was also listed as ARA 100, arasine and GP 1 110. The body makes it naturally.
Sources: Animal study (mice). Tukhovskaya EA et al. AICAR Improves Outcomes of Metabolic Syndrome and Type 2 Diabetes Induced by High-Fat Diet in C57Bl/6 Male Mice. International Journal of Molecular Sciences, 11 December 2022. PMID 36555360. Supports: full name of AICAR, AMPK activator, body weight and liver findings in mice; Lab method study (anti-doping). Buisson C et al. Implementation of AICAR analysis by GC-C-IRMS for anti-doping purposes. Drug Testing and Analysis, November 2017. PMID 29032594. Supports: naturally occurring, on the WADA Prohibited List, claimed performance effect; Drug profile (review). Acadesine: AICA riboside, ARA 100, arasine, GP 1 110. Drugs in R&D, 2008. PMID 18457469. Supports: other names; development for ischaemia-reperfusion injury and chronic lymphocytic leukaemia
What AICAR Does: AMPK
AICAR switches on AMPK. AMPK is an enzyme that senses how much energy a cell has. A 2008 review says the drug form also raises adenosine levels. It says many of its effects on metabolism come partly through AMPK.
The body changes it fast. In a drip study in people, blood levels went up. Red blood cells then took it in quickly and turned it into ZMP. For a peptide also discussed for metabolism, see the MOTS-c profile.
Sources: Human study. Bosselaar M et al. Intravenous AICAR during hyperinsulinemia induces systemic hemodynamic changes but has no local metabolic effect. Journal of Clinical Pharmacology, October 2011. PMID 21148051. Supports: heart rate, blood pressure, conversion to ZMP; Review. Drew BG et al. Acadesine, an adenosine-regulating agent with the potential for widespread indications. Expert Opinion on Pharmacotherapy, August 2008. PMID 18671468. Supports: adenosine and AMPK effects, poor oral bioavailability
Does AICAR Really Work? The Human Data First
In people, the effects found so far are small or missing. In mice, they are large. The table shows the human studies first, then the mouse studies.
| Studied in | Record | What was given | What was reported |
|---|---|---|---|
| Healthy men | Human study, PMID 17513706 (2007) | Short-term AICAR | Muscle sugar uptake rose for a short time; minor effect on the whole body |
| People, by drip into a vein | Human study, PMID 21148051 (2011) | AICAR during high insulin | No direct effect on sugar uptake; heart rate up, blood pressure down |
| Heart bypass patients | RED-CABG randomized trial, PMID 22782417 (2012) | Acadesine in the RED-CABG trial | Did not lower death, stroke or severe heart pumping problems; stopped early |
| Mice that did not exercise | Mouse study, PMID 18674809 (2008) | 4 weeks of AICAR | Metabolic genes turned on; running endurance up 44% |
| Mice on a high-fat diet | Mouse study, PMID 36555360 (2022) | AICAR treatment | Lower body weight and less belly fat |
In people
In healthy men, AICAR raised sugar uptake into muscle for a short time. The effect on the whole body was minor. A later drip study found no direct effect on sugar uptake. It did raise heart rate and lower blood pressure.
In mice
This is where the big claims come from. In mice that did not exercise, 4 weeks of AICAR switched on metabolic genes. They ran 44% longer. That is why AICAR gets called an exercise mimetic. In mice on a high-fat diet, it lowered body weight and belly fat. None of this has been shown in people.
Sources: Human study. Cuthbertson DJ et al. 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men. Diabetes, August 2007. PMID 17513706. Supports: short-term muscle glucose uptake in people; Human study. Bosselaar M et al. Intravenous AICAR during hyperinsulinemia induces systemic hemodynamic changes but has no local metabolic effect. Journal of Clinical Pharmacology, October 2011. PMID 21148051. Supports: heart rate, blood pressure, conversion to ZMP; Human trial (randomized). Newman MF et al. Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial. JAMA, 11 July 2012. PMID 22782417. Supports: stopped for futility; no effect on the main outcome; Animal study (mice). Narkar VA et al. AMPK and PPARdelta agonists are exercise mimetics. Cell, 8 August 2008. PMID 18674809. Supports: 4 weeks of AICAR raised running endurance in sedentary mice; Animal study (mice). Tukhovskaya EA et al. AICAR Improves Outcomes of Metabolic Syndrome and Type 2 Diabetes Induced by High-Fat Diet in C57Bl/6 Male Mice. International Journal of Molecular Sciences, 11 December 2022. PMID 36555360. Supports: full name of AICAR, AMPK activator, body weight and liver findings in mice
Endurance, Fat Loss and Blood Sugar: What Was Tested
AICAR is claimed to boost performance, but that has not been shown in people. The endurance and fat loss results come from mice, and the blood sugar results from small human studies.
- Endurance: tested in mice, which ran 44% longer. Not shown in people.
- Fat loss: tested in mice on a high-fat diet, which lost weight and belly fat. No human fat loss study was found.
- Insulin sensitivity and blood sugar: tested in people. Muscle sugar uptake rose for a short time, with a minor effect on the whole body. During high insulin, a drip study found no direct effect on sugar uptake.
- Heart protection: tested in people as acadesine during bypass surgery. It did not lower death, stroke or severe heart pumping problems.
Sources: Human study. Cuthbertson DJ et al. 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men. Diabetes, August 2007. PMID 17513706. Supports: short-term muscle glucose uptake in people; Human study. Bosselaar M et al. Intravenous AICAR during hyperinsulinemia induces systemic hemodynamic changes but has no local metabolic effect. Journal of Clinical Pharmacology, October 2011. PMID 21148051. Supports: heart rate, blood pressure, conversion to ZMP; Human trial (randomized). Newman MF et al. Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial. JAMA, 11 July 2012. PMID 22782417. Supports: stopped for futility; no effect on the main outcome; Animal study (mice). Tukhovskaya EA et al. AICAR Improves Outcomes of Metabolic Syndrome and Type 2 Diabetes Induced by High-Fat Diet in C57Bl/6 Male Mice. International Journal of Molecular Sciences, 11 December 2022. PMID 36555360. Supports: full name of AICAR, AMPK activator, body weight and liver findings in mice; Lab method study (anti-doping). Buisson C et al. Implementation of AICAR analysis by GC-C-IRMS for anti-doping purposes. Drug Testing and Analysis, November 2017. PMID 29032594. Supports: naturally occurring, on the WADA Prohibited List, claimed performance effect; Animal study (mice). Narkar VA et al. AMPK and PPARdelta agonists are exercise mimetics. Cell, 8 August 2008. PMID 18674809. Supports: 4 weeks of AICAR raised running endurance in sedentary mice
AICAR Dosage
There is no approved human dose of AICAR, and this page gives none. In the human studies, researchers gave it by drip into a vein (PMID 21148051). The 2008 review adds that the drug form is poorly absorbed when swallowed.
Sources: Human study. Bosselaar M et al. Intravenous AICAR during hyperinsulinemia induces systemic hemodynamic changes but has no local metabolic effect. Journal of Clinical Pharmacology, October 2011. PMID 21148051. Supports: heart rate, blood pressure, conversion to ZMP; Review. Drew BG et al. Acadesine, an adenosine-regulating agent with the potential for widespread indications. Expert Opinion on Pharmacotherapy, August 2008. PMID 18671468. Supports: adenosine and AMPK effects, poor oral bioavailability
Why Is AICAR Banned?
AICAR is banned in sport because it is on the WADA Prohibited List. Anti-doping researchers say it is claimed to boost physical performance as a supplement. The body also makes AICAR. So labs measure it in urine with a method called isotope ratio mass spectrometry. A 2026 paper describes a faster version of that test.
Sources: Lab method study (anti-doping). Buisson C et al. Implementation of AICAR analysis by GC-C-IRMS for anti-doping purposes. Drug Testing and Analysis, November 2017. PMID 29032594. Supports: naturally occurring, on the WADA Prohibited List, claimed performance effect; Lab method study (anti-doping). Polet M et al. Rapid Analysis of Urinary AICAR by Liquid Chromatography-Isotope Ratio Mass Spectrometry. Analytical Chemistry, 21 April 2026. PMID 41955491. Supports: prohibited in sports under WADA rules
AICAR as a Drug: The Acadesine Trials
No approval for acadesine was found. It was developed for two uses. One was damage when blood flow returns to tissue, called ischaemia-reperfusion injury. The other was chronic lymphocytic leukaemia.
Its biggest test was the RED-CABG trial in heart bypass surgery. A planned check showed it was very unlikely to succeed. So the trial stopped after 3080 of the planned 7500 people joined. Acadesine did not lower the combined risk of death, nonfatal stroke or severe left ventricular dysfunction. The 2008 review also says acadesine is poorly absorbed when swallowed. It says this rules out some of the uses it discusses.
Sources: Human trial (randomized). Newman MF et al. Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial. JAMA, 11 July 2012. PMID 22782417. Supports: stopped for futility; no effect on the main outcome; Drug profile (review). Acadesine: AICA riboside, ARA 100, arasine, GP 1 110. Drugs in R&D, 2008. PMID 18457469. Supports: other names; development for ischaemia-reperfusion injury and chronic lymphocytic leukaemia; Review. Drew BG et al. Acadesine, an adenosine-regulating agent with the potential for widespread indications. Expert Opinion on Pharmacotherapy, August 2008. PMID 18671468. Supports: adenosine and AMPK effects, poor oral bioavailability
AICAR Side Effects
The human data point to the heart and blood vessels. In a drip study, AICAR raised heart rate and lowered blood pressure. The authors think this was most likely from wider blood vessels.
In a 2022 mouse study, some liver toxic effects were seen. This was in mice on a normal diet that got AICAR from the first day.
No long-term human safety data and no FDA label were found. This page gives no dose, because there is no approved dose. For general risks, see peptide side effects.
Sources: Human study. Bosselaar M et al. Intravenous AICAR during hyperinsulinemia induces systemic hemodynamic changes but has no local metabolic effect. Journal of Clinical Pharmacology, October 2011. PMID 21148051. Supports: heart rate, blood pressure, conversion to ZMP; Animal study (mice). Tukhovskaya EA et al. AICAR Improves Outcomes of Metabolic Syndrome and Type 2 Diabetes Induced by High-Fat Diet in C57Bl/6 Male Mice. International Journal of Molecular Sciences, 11 December 2022. PMID 36555360. Supports: full name of AICAR, AMPK activator, body weight and liver findings in mice
Common Questions
Does AICAR peptide really work?+
In people, only weakly so far. It raised muscle sugar uptake for a short time, with a minor effect on the whole body. A drip study saw no direct effect on sugar uptake. A large heart surgery trial of the drug form, acadesine, was stopped early. In mice, 4 weeks of AICAR raised running endurance by 44%.
Why is AICAR banned?+
AICAR is on the World Anti-Doping Agency (WADA) Prohibited List, so it is banned in sport. Anti-doping researchers note it is claimed to improve physical performance when taken as a supplement. The body also makes AICAR naturally, and anti-doping labs test urine for it with isotope ratio mass spectrometry.
What are the potential side effects of taking AICAR?+
In a human drip study, AICAR raised heart rate and lowered blood pressure. This was most likely from wider blood vessels. In mice on a normal diet given AICAR from day one, some liver toxic effects were seen. No long-term human safety data were found.
Is AICAR a peptide?+
No. Its full name, 5-aminoimidazole-4-carboxamide ribonucleoside, shows it is a ribonucleoside, which is built on a ribose sugar. A peptide is a chain of amino acids, and AICAR has none.
How does AICAR work?+
AICAR turns on AMPK, an enzyme that senses the cell's energy level. A 2008 review says the drug form, acadesine, also raises adenosine levels. In people, red blood cells quickly take up AICAR and turn it into ZMP.
Does AICAR help with fat loss?+
Only in mice so far. In mice fed a high-fat diet, AICAR lowered body weight and the amount of belly fat. No human fat loss study was found, and the same mouse study saw some liver toxic effects in mice on a normal diet.
Sources: Human study. Cuthbertson DJ et al. 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake in healthy men. Diabetes, August 2007. PMID 17513706. Supports: short-term muscle glucose uptake in people; Human study. Bosselaar M et al. Intravenous AICAR during hyperinsulinemia induces systemic hemodynamic changes but has no local metabolic effect. Journal of Clinical Pharmacology, October 2011. PMID 21148051. Supports: heart rate, blood pressure, conversion to ZMP; Human trial (randomized). Newman MF et al. Effect of adenosine-regulating agent acadesine on morbidity and mortality associated with coronary artery bypass grafting: the RED-CABG randomized controlled trial. JAMA, 11 July 2012. PMID 22782417. Supports: stopped for futility; no effect on the main outcome; Animal study (mice). Narkar VA et al. AMPK and PPARdelta agonists are exercise mimetics. Cell, 8 August 2008. PMID 18674809. Supports: 4 weeks of AICAR raised running endurance in sedentary mice; Lab method study (anti-doping). Buisson C et al. Implementation of AICAR analysis by GC-C-IRMS for anti-doping purposes. Drug Testing and Analysis, November 2017. PMID 29032594. Supports: naturally occurring, on the WADA Prohibited List, claimed performance effect; Animal study (mice). Tukhovskaya EA et al. AICAR Improves Outcomes of Metabolic Syndrome and Type 2 Diabetes Induced by High-Fat Diet in C57Bl/6 Male Mice. International Journal of Molecular Sciences, 11 December 2022. PMID 36555360. Supports: full name of AICAR, AMPK activator, body weight and liver findings in mice; Review. Drew BG et al. Acadesine, an adenosine-regulating agent with the potential for widespread indications. Expert Opinion on Pharmacotherapy, August 2008. PMID 18671468. Supports: adenosine and AMPK effects, poor oral bioavailability
Related reading
This guide is for educational purposes only and is not medical advice. It describes what published mouse studies, human studies and anti-doping research report about AICAR and acadesine. It is not an endorsement or an instruction to use any compound. AICAR is not approved for human use and is prohibited in sport. Talk to a qualified healthcare professional before making any decision about your health.