Description
Telmisartan is a long-acting antagonist at angiotensin II type 1 (AT II) receptors that is clinically used to treat hypertension. Telmisartan exhibits antihypertensive, anti-diabetic, anti-obesity, anti-inflammatory, and anti-hyperlipidemic activities. Telmisartan decreases levels of total cholesterol and LDL in vivo. Telmisartan also decreases weight gain and increases activity endurance and oxygen consumption in other animal models. This compound is also a selective modulator of PPARγ/δ, decreasing insulin, glucose, and triglyceride levels in high fat diet-fed rats. In endothelial cells, telmisartan decreases expression of MCP-1 and VCAM-1 and prevents activation of NF-κB.
References
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Feng X, Luo Z, Ma L, et al. Angiotensin II receptor blocker telmisartan enhances running endurance of skeletal muscle through activation of the PPAR-δ/AMPK pathway. J Cell Mol Med. 2011 Jul;15(7):1572-81. PMID: 20477906.
Inoue T, Taguchi I, Abe S, et al. Inhibition of intestinal cholesterol absorption might explain cholesterol-lowering effect of telmisartan. J Clin Pharm Ther. 2011 Feb;36(1):103-10. PMID: 21198725.
Benson SC, Pershadsingh HA, Ho CI, et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension. 2004 May;43(5):993-1002. PMID: 15007034.
Okada M, Kosaka N, Hoshino Y, et al. Effects of captopril and telmisartan on matrix metalloproteinase-2 and -9 expressions and development of left ventricular fibrosis induced by isoprenaline in rats. Biol Pharm Bull. 2010;33(9):1517-1521. PMID: 20823567.
