منابع مشابه
Editorial Commentary Protein Kinase C–Inhibiting Properties of the Losartan Metabolite EXP3179 Make the Difference
The inhibition of the renin-angiotensin axis with the angiotensin II (ATII) receptor blockers, such as losartan, candesartan, and valsartan, has been demonstrated, similar to angiotensin-converting enzyme inhibitors, to reduce mortality in patients with arterial hypertension, chronic congestive heart failure, and acute myocardial infarction.1 Initially, the ATII receptor antagonist losartan hel...
متن کاملLosartan metabolite EXP3179: an AT1-receptor-independent treatment strategy for patients with the metabolic syndrome?
Losartan potassium, the first orally active nonpeptide angiotensin receptor blocker (ARB) to be introduced for clinical use in hypertension, is rapidly absorbed after oral administration, reaching a peak in plasma 1 to 2 hours. Despite being metabolized by the cytochrome P450 (CYP) 3A4, 2C9, and 2C10 isoenzymes, losartan has no clinically relevant interactions with inhibitors and stimulators of...
متن کاملChronic treatment with losartan results in sufficient serum levels of the metabolite EXP3179 for PPARgamma activation.
The losartan metabolite EXP3174 exhibits angiotensin II receptor 1 (AT1R)-blocking properties, whereas the metabolite EXP3179 potently induces the activity of the insulin-sensitizing peroxisome proliferator-activated receptor gamma (PPARgamma) as a partial agonist in vitro. We investigated whether chronic treatment with losartan leads to sufficient serum levels of EXP3179 to activate PPARgamma ...
متن کاملAngiotensin II receptor-independent antiinflammatory and antiaggregatory properties of losartan: role of the active metabolite EXP3179.
Angiotensin II (Ang II) type 1 receptor (AT(1)) antagonists such as losartan (LOS) are widely used for the treatment of hypertension and elicit antiinflammatory and antiaggregatory in vitro and in patients, although the underlying mechanism are unclear. Following computer-based molecule similarity, we proposed that on cytochrome-P450 degradation, the LOS metabolite EXP3179 is generated, which s...
متن کاملProtein kinase C-inhibiting properties of the losartan metabolite EXP3179 make the difference.
The inhibition of the renin-angiotensin axis with the angiotensin II (ATII) receptor blockers, such as losartan, candesartan, and valsartan, has been demonstrated, similar to angiotensin-converting enzyme inhibitors, to reduce mortality in patients with arterial hypertension, chronic congestive heart failure, and acute myocardial infarction.1 Initially, the ATII receptor antagonist losartan hel...
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ژورنال
عنوان ژورنال: Hypertension
سال: 2009
ISSN: 0194-911X,1524-4563
DOI: 10.1161/hypertensionaha.109.138883