AdipoRon

AdipoRon

Systematic (IUPAC) name
2-(4-Benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
Clinical data
Routes of administration	Oral
Identifiers
CAS Number	924416-43-3
ATC code	None
PubChem	CID: 16307093
ChemSpider	11029953
Chemical data
Formula	C27H28N2O3
Molecular mass	428.52282 g/mol
SMILES C1CN(CCC1NC(=O)COC2=CC=C(C=C2)C(=O)C3=CC=CC=C3)CC4=CC=CC=C4

AdipoRon is a selective, orally active, synthetic small-molecule agonist of the adiponectin receptor 1 (AdipoR1) and adiponectin receptor 2 (AdipoR2) (K_d = 1.8 μM and 3.1 μM, respectively). It activates AMPK and PPARα signaling and ameliorates insulin resistance, dyslipidemia, and glucose intolerance in db/db mice (an animal model for type II diabetes and obesity). Moreover, AdipoRon has been found to extend the lifespans of db/db mice fed a high-fat diet, as well as improve exercise endurance. The compound was discovered by Japanese researchers in 2013 via screening of a compound library, and is the first orally active, small-molecule agonist of the adiponectin receptors to be identified.

Adiponectin receptor agonists such as AdipoRon have attracted interest as potential therapies for obesity, diabetes, cardiovascular disease, non-alcoholic fatty liver disease, and a panoply of other conditions. In addition, adiponectin has recently been elucidated to mediate the antidepressant, anxiolytic, and neurogenic effects of physical exercise. Dysregulation of adiponectin expression has also been implicated in the pathology of mood disorders, anxiety disorders, eating disorders, neurodegenerative disorders, and various other neuropsychiatric disorders. Also, it has been determined that exercise improves insulin resistance via activation of AdipoR1. As such, adiponectin receptor agonists are a highly interesting therapeutic target for a variety of different conditions. Moreover, it has been suggested they could potentially be used as a substitute for exercise to achieve similar physical and mental health benefits.