Abbildung 7: Telmisartan - PPAR-Gamma
PPAR-g agonists can improve insulin sensitivity, reduce triglyceride levels and decrease the risk for atherosclerosis. This study examined the ability of different ARBs to activate PPAR-g in a cell-based transient transfection assay.1 This assay eliminates interference from endogenous nuclear receptors. In the results shown here, each ARB was applied at 10 mmol/L. Telmisartan was the only ARB to show strong (27-fold) activation, although irbesartan showed a slight activation (two- to three-fold). By comparison, full PPAR-g agonists show ~140-fold activation in this assay.1 Telmisartan was also the only ARB that activated PPAR-g when tested at lower concentrations that can be achieved physiologically (1–5 mmol/L).1 Telmisartan therefore acts as a partial agonist of PPAR-g. 1. Benson SC, Pershadsingh HA, Ho CI et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARg-modulating activity. Hypertension 2004; 43: 993–1002.