Description
Losartan is an inhibitor of the angiotensin II type 1 (AT1) receptor that exhibits antihypertensive, anti-fibrotic, and nephroprotective activities. In animal models of obstructive nephropathy, losartan decreases levels of α-SMA and collagen type 1 and inhibits phosphorylation of STAT3, suppressing renal tubular fibrosis. Losartan also inhibits the endothelial-to-mesenchymal transition through indirect inhibition of ERK activation, potentially showing anti-fibrotic benefit after myocardial infarction.
References
He P, Li D, Zhang B. Losartan attenuates renal interstitial fibrosis and tubular cell apoptosis in a rat model of obstructive nephropathy. Mol Med Rep. 2014 Aug;10(2):638-44. PMID: 24912579.
Wylie-Sears J, Levine RA, Bischoff J. Losartan inhibits endothelial-to-mesenchymal transformation in mitral valve endothelial cells by blocking transforming growth factor-β-induced phosphorylation of ERK. Biochem Biophys Res Commun. 2014 Apr 18;446(4):870-5. PMID: 24632204.
Gibson TJ. Hypertension, its treatment, hyperuricaemia and gout. Curr Opin Rheumatol. 2013 Mar;25(2):217-22. PMID: 23370375.
Apostolakis S, Krambovitis E, Vlata Z, et al. CX3CR1 receptor is up-regulated in monocytes of coronary artery diseased patients: impact of pre-inflammatory stimuli and renin-angiotensin system modulators. Thromb Res. 2007;121(3):387-395. PMID: 17521710.
Koseki N, Deguchi J, Yamashita A, et al. Establishment fo a novel experimental protocol for drug-induced seizure liability screening based on a locomotor activity assay in zebrafish. J Toxicol Sci. 2014 Aug;39(4):579-600. PMID: 25056783.
Nagata T, Fukuzawa T, Takeda M, et al. Tofogliflozin, a novel sodium-glucose co-transporter 2 inhibitor, improves renal and pancreatic function in db/db mice. Br J Pharmacol. 2013 Oct;170(3):519-531. PMID: 23751087.
