AICAR
Acadesine · 5-Aminoimidazole-4-carboxamide ribonucleotide
AMPK-activating nucleotide studied as an exercise mimetic for endurance and metabolic research.
Key takeaways
- AMPK activator; the exercise-mimetic claim rests on one 2008 mouse study in Cell.
- Human trials happened only for cardiac surgery ischemia (as acadesine), and the big one failed.
- Plotter half-life (~5 hours) is a research estimate, not a human measurement.
- WADA-prohibited; WADA has set urinary thresholds to flag doping versus natural levels.
Reported dosing protocols
Protocols reported in research literature and clinic/community use — informational context, not a dosing recommendation.
| Use case | Dose | Route | Frequency | Duration |
|---|---|---|---|---|
| Cardiac surgery ischemia (clinical trial) | Weight-based IV infusion | IV | Perioperative infusion | Single surgical episode |
| Endurance / metabolic (community) | 10–50 mg | SubQ | Once daily | 4–8 weeks |
Pharmacokinetic summary
- Model tier
- Simple (t½ + F, Tmax estimated)
- Half-life
- 4.8 hours
- Bioavailability
- 50%
- Typical dose
- 10–50 mg
Frequently asked questions
Does AICAR actually improve endurance in humans?
Nobody knows. The exercise-mimetic claim comes from a 2008 study in sedentary mice, and no human efficacy trial has been run for endurance or metabolic use. The only human trials targeted cardiac surgery ischemia, where the drug failed its endpoint.
Is AICAR the same as acadesine?
Yes. Acadesine is the drug-candidate name for AICAR. It reached large cardiac surgery trials under that name but was never approved, so anything sold today is research-chemical grade.
Will AICAR show up on a drug test?
Yes. WADA prohibits AMPK activators under S4.4.1 and detects AICAR in urine by LC-MS. Because AICAR occurs naturally at low levels, WADA research has established thresholds to separate doping from endogenous production.
References
- Estimated (preclinical) — AMPK activator ("exercise in a pill"); human PK limited. Narkar et al. 2008 Cell.
- Narkar et al., Cell 2008 — AMPK and PPARδ agonists are exercise mimetics — The mouse study behind the exercise-mimetic reputation.
- Newman et al., JAMA 2012 — acadesine in coronary artery bypass surgery (RED-CABG) — Large cardiac-surgery trial; acadesine did not reduce the composite endpoint.
- WADA technical documents index — Prohibited-list framework and detection documents covering AMPK activators (S4.4.1).
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