|Chemical and physical data|
|Molar mass||428.52282 g/mol g·mol−1|
|3D model (JSmol)|
AdipoRon is a selective, orally active, synthetic small-molecule agonist of the adiponectin receptor 1 (AdipoR1) and adiponectin receptor 2 (AdipoR2) (Kd = 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.
In 2016, the University of Tokyo announced it was launching an investigation into anonymously made claims of fabricated and falsified data on the identification of AdipoR1, AdipoR2 and AdipoRon.
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- Okada-Iwabu M, Iwabu M, Ueki K, Yamauchi T, Kadowaki T (2015). "Perspective of Small-Molecule AdipoR Agonist for Type 2 Diabetes and Short Life in Obesity". Diabetes Metab J. 39 (5): 363–72. doi:10.4093/dmj.2015.39.5.363. PMC 4641965. PMID 26566493.
- Yau SY, Li A, Hoo RL, Ching YP, Christie BR, Lee TM, Xu A, So KF (2014). "Physical exercise-induced hippocampal neurogenesis and antidepressant effects are mediated by the adipocyte hormone adiponectin". Proc. Natl. Acad. Sci. U.S.A. 111 (44): 15810–5. doi:10.1073/pnas.1415219111. PMC 4226125. PMID 25331877.
- Nicolas S, Veyssière J, Gandin C, Zsürger N, Pietri M, Heurteaux C, Glaichenhaus N, Petit-Paitel A, Chabry J (2015). "Neurogenesis-independent antidepressant-like effects of enriched environment is dependent on adiponectin". Psychoneuroendocrinology. 57: 72–83. doi:10.1016/j.psyneuen.2015.03.017. PMID 25889841.
- Li A, Yau SY, Machado S, Yuan TF, So KF (2015). "Adult neurogenic and antidepressant effects of adiponectin: a potential replacement for exercise?". CNS Neurol Disord Drug Targets. 14 (9): 1129–1144. doi:10.2174/1871527315666151111125533.
- Wędrychowicz, Andrzej (2014). "Peptides from adipose tissue in mental disorders". World Journal of Psychiatry. 4 (4): 103–111. doi:10.5498/wjp.v4.i4.103. ISSN 2220-3206. PMC 4274582. PMID 25540725.
- Cho JK, Kim S, Hong HR, Yoon JH, Kang H (2015). "Exercise Training Improves Whole Body Insulin Resistance via Adiponectin Receptor 1". Int J Sports Med. 36 (13): e24–e30. doi:10.1055/s-0035-1559715. PMID 26528942.
- Yau SY, Li A, Xu A, So KF (2015). "Fat cell-secreted adiponectin mediates physical exercise-induced hippocampal neurogenesis: an alternative anti-depressive treatment?". Neural Regen Res. 10 (1): 7–9. doi:10.4103/1673-5374.150637. PMC 4357120. PMID 25788905.
- University of Tokyo to investigate data manipulation charges against six prominent research groups ScienceInsider, Dennis Normile, Sep 20, 2016
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