Potent insulin sensitizer

A wide spectrum of thiazolidinedione compounds have been synthesized and characterized over the past 15 years. In general, these compounds were shown to be active in obese rodent models of type 2 diabetes but were not active in insulin-deficient diabetes, as in streptozo-tocin-treated rats. Thus, the compounds were shown to be insulin sensitizers with little or no potential to evoke hypoglycemia. In addition to potent insulin-sensitizing and glucose-lowering effects, the thiazolidinediones also showed substantial efficacy with respect to hypertriglyceridemia in animal models. A small number of thiazolidinediones have... 

LT175, a novel peroxisome proliferator-activated receptor alpha/gamma (PPARa/y) ligand with potent insulin-sensitizing effects and reduced adipogenic properties. 

Cox PJ, Ryan DA, Hollis FJ, et al. Absorption, disposition, and metabolism of rosiglitazone, a potent thiazolidinedione insulin sensitizer, in humans. Drug Metab Dispos 2000 28 772-780. 

As seen in Fig. 3, blood glucose values during triple therapy were not completely normalised during the 24-h period. This may be explained by insulin resistance, since our euglycaemic hyperin-sulinaemic clamp studies showed an improvement only in peripheral insulin sensitivity of about 60%. Therefore, to completely normalise blood glucose values, a more potent insulin synthesizer than rosiglitazone is needed. 

Cox, P.J. Ryan, D.A. Hollis, F.J. Harris, A.-M. Miller, A.K. Vousden, M. Cowley, H. Absorption, disposition, and metabolism of rosiglitazone, a potent thiazohdinedione insulin sensitizer, in humans. Drug Metab.Dispos., 2000,28, 772-780. [plasma urine feces UV detection LC-MS SPE]... 

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