The mechanism by which drugs inhibit organic anion transporter 1 (OAT1) was examined. OAT1 was stably expressed in Chinese hamster ovary (CHO) cells, and para-aminohippurate (PAH) and 6-carboxyfluorescein were the substrates. Most compounds (10 of 14) inhibited competitively, increasing the Michaelis constant (Km) without affecting the maximal transport rate (Jmax). Others were mixed-type (lowe...

BACKGROUND Endothelium has a function to regulate vascular tone by releasing mediators either vasodilating or vasoconstricting blood vessels. Endothelial dysfunction can be measured conveniently by Reactive Hyperemia Index (RHI) with a peripheral arterial tonometry. Angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin II (AT II) receptor blockers (ARBs) are considered to have benefi...

BACKGROUND AND OBJECTIVES Several studies have shown that angiotensin II receptor blockers (ARBs) improve endothelial function and arterial stiffness. Telmisartan is a highly selective ARB that activates peroxisome proliferator-activated receptor gamma (PPARgamma). The purpose of this study was to evaluate the effects of telmisartan, such as endothelial function, arterial stiffness, and insulin...

We investigated the ability of angiotensin II type 1 (AT1) receptor blockers with peroxisome proliferator-activated receptor (PPAR)-gamma agonist activity (telmisartan and irbesartan) and AT1 receptor blockers devoid of PPARgamma agonist activity (eprosartan and valsartan) to inhibit vascular cell proliferation studied in the absence of angiotensin II stimulation. Telmisartan and, to a lesser e...

Telmisartan, in addition to blocking angiotensin (Ang) II type 1 receptor (AT1R), activates peroxisome proliferator activated receptor (PPAR ) signaling that interferes with nitric oxide (NO) system. Because aging of endothelial cells (ECs) is hallmarked by a reduction in NO synthesis, we hypothesized that telmisartan increases NO formation by regulated asymmetrical dimethylarginine (ADMA)-dime...

BACKGROUND We investigated the potential of telmisartan to improve microvascular dysfunction induced by myocardial ischemia/reperfusion (I/R) injury by activating the peroxisome proliferator-activated receptor gamma (PPARG) pathway. METHODS Forty-eight male rabbits were randomly allocated into sham-operated, I/R, GW9662, telmisartan, telmisartan-GW9662, or candesartan groups. Rabbits were ane...

AIMS Telmisartan activates peroxisome proliferator-activated receptor-γ (PPARγ) in addition to serving as an angiotensin II type 1 receptor (AT(1)R) blocker. The PPARγ activity of telmisartan on resistance arteries has remained largely unknown. The present study investigated the hypothesis that telmisartan inhibited vascular tension in mouse mesenteric resistance arteries, which was attributed ...

The present study aimed to investigate the delayed protective effect of telmisartan on lung ischemic/reperfusion injury in patients undergoing heart valve replacement operations. In total, 180 patients diagnosed with rheumatic valve diseases were randomly divided into the telmisartan (T), captopril (C) and placebo (P) groups. In the telmisartan group, the patients were pretreated with telmisart...

Angiotensin type-1 receptor blockers (ARBs) are being one of the first-line treatments for hypertension. Despite the availability of various types of ARBs, there are no comparative studies of their effects in North Indian patients. In this open-label, prospective, randomized study, we compared the antihypertensive effects of olmesartan (20 mg/day) versus telmisartan (40 mg/day) in newly diagnos...

AIM This study compared the effects of telmisartan and losartan on nonalcoholic fatty liver disease (NAFLD) and biochemical markers of insulin resistance in hypertensive NAFLD patients with type 2 diabetes mellitus. METHODS This was a randomized, open-label, parallel-group comparison of therapy with telmisartan or losartan. Nineteen hypertensive NAFLD patients with type 2 diabetes were random...