Endothelin-1 Receptors in Rat Tissues: Characterization by Bosentan, Ambrisentan and CI-1020
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- Yokoyama Yoshinari
- Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka Department of Clinical Pharmacology and Genetics, School of Pharmaceutical Sciences, University of Shizuoka
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- Osano Ayaka
- Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka Department of Clinical Pharmacology and Genetics, School of Pharmaceutical Sciences, University of Shizuoka
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- Hayashi Hideki
- Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka Department of Clinical Pharmacology and Genetics, School of Pharmaceutical Sciences, University of Shizuoka
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- Itoh Kunihiko
- Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka Department of Clinical Pharmacology and Genetics, School of Pharmaceutical Sciences, University of Shizuoka
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- Okura Takashi
- Laboratory of Drug Disposition & Pharmacokinetics, Faculty of Pharma-Science, Teikyo University
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- Deguchi Yoshiharu
- Laboratory of Drug Disposition & Pharmacokinetics, Faculty of Pharma-Science, Teikyo University
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- Ito Yoshihiko
- Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka Department of Clinical Pharmacology and Genetics, School of Pharmaceutical Sciences, University of Shizuoka
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- Yamada Shizuo
- Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka Department of Clinical Pharmacology and Genetics, School of Pharmaceutical Sciences, University of Shizuoka
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The present study aimed to characterize comparatively endothelin-1 (ET-1) receptors in rat tissues by radioligand binding assay using [125I]ET-1 and to examine receptor binding after oral administration of bosentan. Significant amount of specific [125I]ET-1 binding was detected in the lung, heart, kidney, bladder and cerebral cortex of rats. ET-1, bosentan, ambrisentan, and CI-1020 inhibited specific [125I]ET-1 binding in these tissues in a concentration-dependent manner. The Hill coefficients of each agent in the rat lung and cerebral cortex and those of bosentan and ET-1 in the heart, kidney and bladder were close to unity, while the Hill coefficients of ambrisentan and CI-1020 in the heart, kidney and bladder were less than one. The nonlinear least squares regression analysis revealed the presence of high- and low-affinity ET-1 receptor sites in these tissues for ambrisentan and CI-1020. Oral administration of bosentan caused a dose-dependent decrease in specific [125I]ET-1 binding in the rat lung, kidney and bladder, suggesting significant binding of the tissue ET-1 receptors in vivo. In conclusion, it has been shown that a significant amount of pharmacologically relevant ET-1 receptors may exist in rat tissues and that ET-1 receptor antagonists such as bosentan at pharmacological doses may exert some pharmacological effects by binding these ET-1 receptors.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 37 (3), 461-465, 2014
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679609931136
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- NII論文ID
- 130003390952
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- NII書誌ID
- AA10885497
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- COI
- 1:STN:280:DC%2BC2cvpsFOgtg%3D%3D
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 025297791
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- PubMed
- 24583865
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可