PMID: 22358092Feb 24, 2012Paper

Novel I1-imidazoline S43126 enhance insulin action in PC12 cells

Pharmacological Reports : PR
Jerusalem TesfaiL Edwards

Abstract

The I(1)-imidazoline receptor is a novel target for drug development for hypertension and insulin resistance, major disorders associated with type 2 diabetes. In the present study, we examined the effects of a novel imidazoline agonist S43126, on phosphorylation of protein kinase B (PKB/Akt) and extracellular signal-regulated kinase (ERK1/2) in PC12 cells. We further examined the effects of S43126 on insulin stimulated PKB and ERK phosphorylation. PC12 cells were treated with varying doses of S43126 (10(-10) to 10(-6) M) or insulin (10(-10) to 10(-6) M) or combination treatment with insulin (10(-6) M) and varying doses of S43126 (10(-6) - 10(-11) M) for 10 min. Western blot analysis of treated samples showed that S43126 increased both ERK1/2 and PKB phosphorylation by 5 fold. Combination treatment with insulin (10(-6) M) and varying doses of S43126 (10(-6) - 10(-11) M) enhanced phosphorylation of PKB and ERK1/2 above the level of insulin alone, in a dose and time dependent manner. Treatment with siRNA against Nischarin (mouse homologue of I(1)-imidazoline receptor) reduced the phosphorylation of both ERK and PKB following combination treatments. These results indicate that S43126 has the potential to augment insulin action and ...Continue Reading

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Citations

Jul 19, 2014·European Journal of Pharmacology·Henry AcerosSuhayla Mukaddam-Daher
Jan 16, 2016·Chemical Research in Toxicology·Owen R KinskySerrine S Lau
Mar 29, 2014·Clinical Toxicology : the Official Journal of the American Academy of Clinical Toxicology and European Association of Poisons Centres and Clinical Toxicologists·J A Lowry, J T Brown

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