Telmisartan Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. In vitro
Telmisartan functions as a moderately potent (EC50=4.5 μM), selective PPARγ partial agonist, activating the receptor to 25% to 30% of the maximum level achieved by the full agonists pioglitazone and rosiglitazone. Telmisartan induces adipocyte differentiation of 3T3-L1 cells. Telmisartan causes a 60% to 70% decrease in the expression of ACC2 in murine muscle myotubes. Telmisartan, but not candesartan, another ARB, downregulates RAGE mRNA levels in a dose-dependent manner. Telmisartan decreases basal as well as AGE-induced RAGE protein expression in Hep3B cells. Telmisartan dose-dependently inhibits AGE-induced ROS generation and subsequent CRP gene and protein induction in Hep3B cells. Telmisartan effectively facilitates differentiation of 3T3-L1 preadipocytes. Telmisartan causes a dose-dependent increase in mRNA levels for PPARgamma target genes such as aP2 and adiponectin in both differentiating adipocytes and fully differentiated adipocytes. Telmisartan attenuates 11beta-hydroxysteroid dehydrogenase type 1 mRNA level in differentiated adipocytes.
In vivo
Telmisartan promotes increases in caloric expenditure and protects against dietary-induced weight gain in rats fed with a high-fat, high-carbohydrate diet. Telmisartan reduces the accumulation of visceral fat and decreases adipocyte size to a much greater extent than valsartan and is also associated with a significant reduction in hepatic triglyceride levels in rats fed with a high-fat, high-carbohydrate diet. Cell Data
