Tamsulosin Potently and Selectively Antagonizes Human Recombinant α₁A/₁D-Adrenoceptors : Slow Dissociation from the α₁A-Adrenoceptor May Account for Selectivity for α₁A-Adrenoceptor over α₁B-Adrenoceptor Subtype
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- Sato Shuichi
- Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Hatanaka Toshiki
- Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Yuyama Hironori
- Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Ukai Masashi
- Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Noguchi Yukiko
- Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Ohtake Akiyoshi
- Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Taguchi Katsunari
- Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Sasamata Masao
- Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
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- Miyata Keiji
- Applied Pharmacology Research Laboratories, Drug Discovery Research, Astellas Pharma Inc.
書誌事項
- タイトル別名
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- Tamsulosin Potently and Selectively Antagonizes Human Recombinant .ALPHA.1A/1D-Adrenoceptors: Slow Dissociation from the .ALPHA.1A-Adrenoceptor May Account for Selectivity for .ALPHA.1A-Adrenoceptor over .ALPHA.1B-Adrenoceptor Subtype
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抄録
We determined the binding affinity of tamsulosin, a selective α1-adrenoceptor antagonist, for human α1-adrenoceptor subtypes in comparison with those of other α1-adrenoceptor antagonists including silodosin, prazosin, 5-methylurapidil, terazosin, alfuzosin, nafopidil, urapidil and BMY7378. The association and dissociation kinetics of [3H]tamsulosin for recombinant human α1-adrenoceptor subtypes were compared with those of [3H]prazosin. Tamsulosin competitively inhibited [3H]prazosin binding to human α1A-, α1B- and α1D-adrenoceptors (pKi values were 10.38, 9.33, 9.85) indicating 11 and 3.4-fold higher affinities for human α1A-adrenoceptor than those for α1B- and α1D-adrenoceptors, respectively. The affinity of tamsulosin for the human α1A-adrenoceptor was, respectively, 5, 9.9, 38, 120, 280, 400, 1200 and 10000 fold higher than those of silodosin, prazosin, 5-methylurapidil, terazosin, alfuzosin, naftopidil, urapidil and BMY7378, respectively. [3H]Tamsulosin dissociated from the α1A-adrenoceptor slower than from the α1B- and α1D-adrenoceptors (α1B>α1D>α1A). Moreover, [3H]tamsulosin dissociated slower than [3H]prazosin from the α1A-adrenoceptor and faster from the α1B- and α1D-adrenoceptors. In conclusion, tamsulosin potently and selectively antagonized α1A/1D-adrenoceptor ligand binding, and slowly dissociated from the α1A-adrenoceptor subtype.
収録刊行物
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- Biological & Pharmaceutical Bulletin
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Biological & Pharmaceutical Bulletin 35 (1), 72-77, 2012
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
- 1390001204632454784
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- NII論文ID
- 130001872345
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- NII書誌ID
- AA10885497
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- COI
- 1:STN:280:DC%2BC387isVCgug%3D%3D
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- ISSN
- 13475215
- 09186158
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- NDL書誌ID
- 024029694
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- PubMed
- 22223340
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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