In Vivo Measurement of 1, 4-Dihydropyridine Receptors in Mesenteric Arteries of Spontaneously Hypertensive Rats and Effect of Nifedipine and Cilnidipine
スポンサーリンク
概要
- 論文の詳細を見る
The present study was undertaken to measure 1, 4-dihydropyridine(DHP)receptor binding sites in vivo in the mesenteric artery and other tissues of spontaneously hypertensive rats(SHR)and to examine the effect of nifedipine and cilnidipine. Specific in vivo binding of(+)-[^3H]PN 200-110 in the SHR mesenteric artery was dose dependently reduced by oral administration of nifedipine at relatively low doses. Oral administration of cilnidipine(6.09 μmol/kg)significantly reduced the specific in vivo binding of(+)-[^3H]PN 200-110 in the mesenteric artery, aorta, and myocardium. A significant reduction in(+)-[^3H]PN 200-110 binding was seen at 1-12 h in the mesenteric artery and at 1-7 h in the aorta and myocardium. In contrast, oral administration of nifedipine(28.9 μmol/kg)markedly reduced in vivo(+)-[^3H]PN 200-110 binding in all tissues of SHR at 1-6 h, and the degree and time course of the reduction did not differ much among the tissues. The area under the curve(AUC)for receptor occupancy vs. time was calculated from the reduction rate(%)of specific in vivo(+)-[^3H]PN 200-110 binding. The ratio(1.4 or 1.7)of the AUC_<mesenteric artery> to AUC_<aorta> or AUC_<myocardium> after oral administration of cilnidipine was greater than the corresponding value(1.1)for nifedipine. In conclusion, the present study demonstrates that cilnidipine, but not nifedipine, may occupy 1, 4-DHP receptors in the small artery in a more selective and sustained manner than in other tissues of SHR, and thus such receptor binding specificity may be responsible for the long-lasting hypotensive effect of this drug.
- 公益社団法人日本薬学会の論文
- 2002-01-01
著者
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山田 幸子
日本大学医学部生化学分野
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山田 静雄
静岡県立大学・薬学部・医療薬学大講座薬物動態学分野
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Yamada S
Department Of Biopharmacy School Of Pharmaceutical Sciences University Of Shizuoka
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木村 良平
静岡県立大学薬学部薬剤学・coe21
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木村 良平
東北大学大学院工学研究科
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木村 良平
静岡県立大学薬学部 薬剤学教室
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Kimura R
School Of Pharmaceutical Sciences And Coe21 University Of Shizuoka Medicine
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YAMADA Shizuo
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, S
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UCHIDA Shinya
Department of Pharmacokinetics and Pharmacodynamics and Global COE Program, School of Pharmaceutical
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Uchida S
Department Of Hospital Pharmacy Hamamatsu University School Of Medicine
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Uchida Shinya
Department Of Biopharmacy School Of Pharmaceutical Sciences University Of Shizuoka
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Uchida Shinya
Department Of Hospital Pharmacy Hamamatsu University School Of Medicine
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木村 良平
静岡県立大学薬学部薬剤学教室
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Uchida Shinya
Department Of Pharmacokinetics And Pharmacodynamics And Global Coe Program School Of Pharmaceuticals
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Uchida Shinya
Department Of Pharmacokinetics And Pharmacodynamics And Global Coe Program School Of Pharmaceutical
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KIMURA Ryohei
Department of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka
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NAKAJIMA Mariko
Department of Biopharmacy, University of Shizuoka School of Pharmaceutical Sciences
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Yamada Shizuo
Department Of Pharmacokinetics And Pharmacodynamics And Global Coe Program School Of Pharmaceutical
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Yamada Shizuo
Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka
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Kimura Ryohei
Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka
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山田 静雄
静岡県立大学 薬学部
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Uchida Shinya
Department Of Anesthesiology Gunma University Hospital
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Nakajima Mariko
Department Of Biopharmacy University Of Shizuoka School Of Pharmaceutical Sciences
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