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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.<ref name="pmid24172895" /><ref name="HollandScherer2013" /> In addition, [[adiponectin]] has recently been elucidated to mediate the [[antidepressant]], [[anxiolytic]], and [[neurogenic]] effects of [[physical exercise]].<ref name="pmid25331877">{{cite journal | vauthors = Yau SY, Li A, Hoo RL, Ching YP, Christie BR, Lee TM, Xu A, So KF | title = Physical exercise-induced hippocampal neurogenesis and antidepressant effects are mediated by the adipocyte hormone adiponectin | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 111 | issue = 44 | pages = 15810–5 | year = 2014 | pmid = 25331877 | pmc = 4226125 | doi = 10.1073/pnas.1415219111 | url = }}</ref><ref name="pmid25889841">{{cite journal | vauthors = Nicolas S, Veyssière J, Gandin C, Zsürger N, Pietri M, Heurteaux C, Glaichenhaus N, Petit-Paitel A, Chabry J | title = Neurogenesis-independent antidepressant-like effects of enriched environment is dependent on adiponectin | journal = Psychoneuroendocrinology | volume = 57 | issue = | pages = 72–83 | year = 2015 | pmid = 25889841 | doi = 10.1016/j.psyneuen.2015.03.017 | url = }}</ref><ref name="Li2015">{{cite journal | vauthors = Li A, Yau SY, Machado S, Yuan TF, So KF | title = Adult neurogenic and antidepressant effects of adiponectin: a potential replacement for exercise? | journal = CNS Neurol Disord Drug Targets | volume = | issue = | pages = | year = 2015 | pmid = | doi = | url = }}</ref> Dysregulation of adiponectin expression has also been implicated in the [[pathology]] of [[mood disorder]]s, [[anxiety disorder]]s, [[eating disorder]]s, [[neurodegenerative disorder]]s, and various other [[neuropsychiatric disorder]]s.<ref name="Wędrychowicz2014">{{cite journal|last1=Wędrychowicz|first1=Andrzej|title=Peptides from adipose tissue in mental disorders|journal=World Journal of Psychiatry|volume=4|issue=4|year=2014|pages=103|issn=2220-3206|doi=10.5498/wjp.v4.i4.103}}</ref> Also, it has been determined that exercise improves [[insulin resistance]] via activation of AdipoR1.<ref name="pmid26528942">{{cite journal | vauthors = Cho JK, Kim S, Hong HR, Yoon JH, Kang H | title = Exercise Training Improves Whole Body Insulin Resistance via Adiponectin Receptor 1 | journal = Int J Sports Med | volume = | issue = | pages = | year = 2015 | pmid = 26528942 | doi = 10.1055/s-0035-1559715 | url = }}</ref> As such, adiponectin receptor agonists are a highly interesting therapeutic target for a variety of different conditions.<ref name="pmid24172895" /><ref name="HollandScherer2013" /><ref name="Li2015" /><ref name="Wędrychowicz2014" /> Moreover, it has been suggested they could potentially be used as a substitute for exercise to achieve similar physical and mental health benefits.<ref name="pmid24172895" /><ref name="HollandScherer2013" /><ref name="Li2015" /><ref name="pmid25788905">{{cite journal | vauthors = Yau SY, Li A, Xu A, So KF | title = Fat cell-secreted adiponectin mediates physical exercise-induced hippocampal neurogenesis: an alternative anti-depressive treatment? | journal = Neural Regen Res | volume = 10 | issue = 1 | pages = 7–9 | year = 2015 | pmid = 25788905 | pmc = 4357120 | doi = 10.4103/1673-5374.150637 | url = }}</ref>
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.<ref name="pmid24172895" /><ref name="HollandScherer2013" /> In addition, [[adiponectin]] has recently been elucidated to mediate the [[antidepressant]], [[anxiolytic]], and [[neurogenic]] effects of [[physical exercise]].<ref name="pmid25331877">{{cite journal | vauthors = Yau SY, Li A, Hoo RL, Ching YP, Christie BR, Lee TM, Xu A, So KF | title = Physical exercise-induced hippocampal neurogenesis and antidepressant effects are mediated by the adipocyte hormone adiponectin | journal = Proc. Natl. Acad. Sci. U.S.A. | volume = 111 | issue = 44 | pages = 15810–5 | year = 2014 | pmid = 25331877 | pmc = 4226125 | doi = 10.1073/pnas.1415219111 | url = }}</ref><ref name="pmid25889841">{{cite journal | vauthors = Nicolas S, Veyssière J, Gandin C, Zsürger N, Pietri M, Heurteaux C, Glaichenhaus N, Petit-Paitel A, Chabry J | title = Neurogenesis-independent antidepressant-like effects of enriched environment is dependent on adiponectin | journal = Psychoneuroendocrinology | volume = 57 | issue = | pages = 72–83 | year = 2015 | pmid = 25889841 | doi = 10.1016/j.psyneuen.2015.03.017 | url = }}</ref><ref name="Li2015">{{cite journal | vauthors = Li A, Yau SY, Machado S, Yuan TF, So KF | title = Adult neurogenic and antidepressant effects of adiponectin: a potential replacement for exercise? | journal = CNS Neurol Disord Drug Targets | volume = | issue = | pages = | year = 2015 | pmid = | doi = | url = }}</ref> Dysregulation of adiponectin expression has also been implicated in the [[pathology]] of [[mood disorder]]s, [[anxiety disorder]]s, [[eating disorder]]s, [[neurodegenerative disorder]]s, and various other [[neuropsychiatric disorder]]s.<ref name="Wędrychowicz2014">{{cite journal|last1=Wędrychowicz|first1=Andrzej|title=Peptides from adipose tissue in mental disorders|journal=World Journal of Psychiatry|volume=4|issue=4|year=2014|pages=103|issn=2220-3206|doi=10.5498/wjp.v4.i4.103}}</ref> Also, it has been determined that exercise improves [[insulin resistance]] via activation of AdipoR1.<ref name="pmid26528942">{{cite journal | vauthors = Cho JK, Kim S, Hong HR, Yoon JH, Kang H | title = Exercise Training Improves Whole Body Insulin Resistance via Adiponectin Receptor 1 | journal = Int J Sports Med | volume = | issue = | pages = | year = 2015 | pmid = 26528942 | doi = 10.1055/s-0035-1559715 | url = }}</ref> As such, adiponectin receptor agonists are a highly interesting therapeutic target for a variety of different conditions.<ref name="pmid24172895" /><ref name="HollandScherer2013" /><ref name="Li2015" /><ref name="Wędrychowicz2014" /> Moreover, it has been suggested they could potentially be used as a substitute for exercise to achieve similar physical and mental health benefits.<ref name="pmid24172895" /><ref name="HollandScherer2013" /><ref name="Li2015" /><ref name="pmid25788905">{{cite journal | vauthors = Yau SY, Li A, Xu A, So KF | title = Fat cell-secreted adiponectin mediates physical exercise-induced hippocampal neurogenesis: an alternative anti-depressive treatment? | journal = Neural Regen Res | volume = 10 | issue = 1 | pages = 7–9 | year = 2015 | pmid = 25788905 | pmc = 4357120 | doi = 10.4103/1673-5374.150637 | url = }}</ref>

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.<ref name="Dennis">[http://www.sciencemag.org/news/2016/09/university-tokyo-investigate-data-manipulation-charges-against-six-prominent-research University of Tokyo to investigate data manipulation charges against six prominent research groups] ScienceInsider, Dennis Normile, Sep 20, 2016</ref>


==References==
==References==

Revision as of 11:34, 13 September 2017

AdipoRon
Clinical data
Routes of
administration
Oral
ATC code
  • None
Identifiers
  • 2-(4-Benzoylphenoxy)-N-(1-benzylpiperidin-4-yl)acetamide
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC27H28N2O3
Molar mass428.52282 g/mol g·mol−1
3D model (JSmol)
  • 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) (Kd = 1.8 μM and 3.1 μM, respectively).[1][2] 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).[1][2] Moreover, AdipoRon has been found to extend the lifespans of db/db mice fed a high-fat diet, as well as improve exercise endurance.[1][2][3] 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.[1][2]

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.[1][2] In addition, adiponectin has recently been elucidated to mediate the antidepressant, anxiolytic, and neurogenic effects of physical exercise.[4][5][6] 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.[7] Also, it has been determined that exercise improves insulin resistance via activation of AdipoR1.[8] As such, adiponectin receptor agonists are a highly interesting therapeutic target for a variety of different conditions.[1][2][6][7] Moreover, it has been suggested they could potentially be used as a substitute for exercise to achieve similar physical and mental health benefits.[1][2][6][9]

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.[10]

References

  1. ^ a b c d e f g Okada-Iwabu M, Yamauchi T, Iwabu M, Honma T, Hamagami K, Matsuda K, Yamaguchi M, Tanabe H, Kimura-Someya T, Shirouzu M, Ogata H, Tokuyama K, Ueki K, Nagano T, Tanaka A, Yokoyama S, Kadowaki T (2013). "A small-molecule AdipoR agonist for type 2 diabetes and short life in obesity". Nature. 503 (7477): 493–9. doi:10.1038/nature12656. PMID 24172895.
  2. ^ a b c d e f g Holland, W. L.; Scherer, P. E. (2013). "Ronning After the Adiponectin Receptors". Science. 342 (6165): 1460–1461. doi:10.1126/science.1249077. ISSN 0036-8075. PMC 4084614. PMID 24357309.
  3. ^ 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.
  4. ^ 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.
  5. ^ 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.
  6. ^ a b c 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.
  7. ^ a b Wędrychowicz, Andrzej (2014). "Peptides from adipose tissue in mental disorders". World Journal of Psychiatry. 4 (4): 103. doi:10.5498/wjp.v4.i4.103. ISSN 2220-3206.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  8. ^ 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. doi:10.1055/s-0035-1559715. PMID 26528942.
  9. ^ 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.{{cite journal}}: CS1 maint: unflagged free DOI (link)
  10. ^ University of Tokyo to investigate data manipulation charges against six prominent research groups ScienceInsider, Dennis Normile, Sep 20, 2016

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