کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5830153 | 1559014 | 2011 | 10 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Antihypertensive, insulin-sensitising and renoprotective effects of a novel, potent and long-acting angiotensin II type 1 receptor blocker, azilsartan medoxomil, in rat and dog models
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
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چکیده انگلیسی
The pharmacological profile of a novel angiotensin II type 1 receptor blocker, azilsartan medoxomil, was compared with that of the potent angiotensin II receptor blocker olmesartan medoxomil. Azilsartan, the active metabolite of azilsartan medoxomil, inhibited the binding of [125I]-Sar1-I1e8-angiotensin II to angiotensin II type 1 receptors. Azilsartan medoxomil inhibited angiotensin II-induced pressor responses in rats, and its inhibitory effects lasted 24 h after oral administration. The inhibitory effects of olmesartan medoxomil disappeared within 24 h. ID50 values were 0.12 and 0.55 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively. In conscious spontaneously hypertensive rats (SHRs), oral administration of 0.1-1 mg/kg azilsartan medoxomil significantly reduced blood pressure at all doses even 24 h after dosing. Oral administration of 0.1-3 mg/kg olmesartan medoxomil also reduced blood pressure; however, only the two highest doses significantly reduced blood pressure 24 h after dosing. ED25 values were 0.41 and 1.3 mg/kg for azilsartan medoxomil and olmesartan medoxomil, respectively. In renal hypertensive dogs, oral administration of 0.1-1 mg/kg azilsartan medoxomil reduced blood pressure more potently and persistently than that of 0.3-3 mg/kg olmesartan medoxomil. In a 2-week study in SHRs, azilsartan medoxomil showed more stable antihypertensive effects than olmesartan medoxomil and improved the glucose infusion rate, an indicator of insulin sensitivity, more potently (â¥Â 10 times) than olmesartan medoxomil. Azilsartan medoxomil also exerted more potent antiproteinuric effects than olmesartan medoxomil in Wistar fatty rats. These results suggest that azilsartan medoxomil is a potent angiotensin II receptor blocker that has an attractive pharmacological profile as an antihypertensive agent.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 669, Issues 1â3, 1 November 2011, Pages 84-93
Journal: European Journal of Pharmacology - Volume 669, Issues 1â3, 1 November 2011, Pages 84-93
نویسندگان
Keiji Kusumoto, Hideki Igata, Mami Ojima, Ayako Tsuboi, Mitsuaki Imanishi, Fuminari Yamaguchi, Hiroki Sakamoto, Takanobu Kuroita, Naohiro Kawaguchi, Nobuhiro Nishigaki, Hideaki Nagaya,