AICAR (Acadesine)

What AICAR Is and What the Studies Measured Studies exploring Adamax have focused on its influence on cognitive performance, neuroprotection, and neurological recovery. Researchers have documented the following areas of interest: Compound Class and Identity AICAR is a nucleoside analogue, not a peptide. Its chemical name is 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside; it is also called acadesine, its international non-proprietary name, and AICA riboside. CAS 2627-69-2, molecular formula C9H14N4O5, molecular weight 258.23. The ATC code C01EB13 was assigned during its clinical development. Supplied as a lyophilised powder in 50mg vials. How It Reaches Its Target AICAR enters cells through adenosine transporters and is phosphorylated by adenosine kinase to AICAR monophosphate, known as ZMP. ZMP is a structural mimic of AMP. It binds the gamma subunit of AMP-activated protein kinase at the nucleotide-binding sites, producing allosteric activation without a genuine change in the cell's AMP to ATP ratio. That two-step route is why the riboside, not the nucleotide, is the compound supplied. What the Landmark Study Measured The paper that made AICAR widely known is Narkar and colleagues, Cell, 2008, titled “AMPK and PPARδ agonists are exercise mimetics”. The model was mice. Measured endpoints included running time and distance to exhaustion on a treadmill, skeletal muscle gene expression, and mitochondrial markers. It is a mouse study. The World Anti-Doping Agency added AICAR to the Prohibited List the following year. Clinical Development and Where It Stopped Unlike most compounds in this catalogue, AICAR reached late-stage human trials. Acadesine was licensed by Schering-Plough from PeriCor Therapeutics and entered the RED-CABG phase 3 trial in 2009, testing prevention of reperfusion injury in coronary artery bypass graft surgery. The trial was terminated in late 2010 on an interim futility analysis. Acadesine has also been explored in haematological malignancy. It holds no approval from the FDA or the EMA.

AMP-activated protein kinase is a heterotrimeric enzyme that responds to the cell’s AMP to ATP ratio and, when activated, shifts metabolism from anabolic to catabolic pathways. It sits upstream of a large number of processes, which is what makes it interesting as a target and also what makes systemic activation difficult to study cleanly.

AICAR has been the standard pharmacological tool for activating AMPK in cell culture and rodent work since the 1990s, and much of what is understood about the enzyme was established using it. That tool status is the compound’s real significance. Published work spans skeletal muscle, liver, adipose tissue, cardiac ischaemia models and haematological cell lines, and the great majority of it is preclinical.

A defined nucleoside analogue with a characterised mechanism, an assigned INN, and a documented clinical trial history.

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