Pioglitazone (112529-15-4) is a clinically useful antidiabetic drug.1 It is a selective agonist of the human peroxisome proliferator-activated receptor γ 1 (PPARγ1; EC50 = 490 nM2, 550 nM3) with weak agonist activity at PPARα and no activity at PPARδ.2 Inhibits mitochondrial pyruvate metabolism and glucose production in hepatocytes.4 Suppresses production of inflammatory cytokines and shows antidepressant-like activity in mouse models.5
References/Citations
1) Merck 14:7452
2) Sakamoto et al. (2000), Activation of human peroxisome proliferator-activated receptor (PPAR) subtypes by pioglitazone; Biochem. Biophys. Res. Commun., 278 704
3) Wilson et al. (2000), The PPARs: From Orphan Receptors to Drug Discovery; J. Med. Chem., 43 527
4) Shannon et al. (2017), Pioglitazone Inhibits Mitochondrial Pyruvate Metabolism and Glucose Production in Hepatocytes; FEBS J., 284 451
5) Zhao et al. (2016), The Antidepressant-Like Effects of Pioglitazone in a Chronic Mild Stress Mouse Model Are Associated With PPARγ-Mediated Alteration of Microglial Activation Phenotypes; Neuroinflamm., 13 259