Blockade by NIP-142, an Antiarrhythmic Agent, of Carbachol-Induced Atrial Action Potential Shortening and GIRK1/4 Channel
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概要
- 論文の詳細を見る
Mechanisms for the atria-specific action potential-prolonging action of NIP-142 ((3R*,4S*)-4-cyclopropylamino-3,4-dihydro-2,2-dimethyl-6-(4-methoxyphenylacetylamino)-7-nitro-2H-1-benzopyran-3-ol), a benzopyran compound that terminates experimental atrial arrhythmia, was examined. In isolated guinea-pig atrial tissue, NIP-142 reversed the shortening of action potential duration induced by either carbachol or adenosine. These effects were mimicked by tertiapin, but not by E-4031. NIP-142 concentration-dependently blocked the human G protein-coupled inwardly rectifying potassium channel current (GIRK1/4 channel current) expressed in HEK-293 cells with an EC50 value of 0.64 μM. At higher concentrations, NIP-142 blocked the human ether a go-go related gene (HERG) channel current with an EC50 value of 44 μM. In isolated guinea-pig papillary muscles, NIP-142 had no effect on the negative inotropic effect of carbachol under β-adrenergic stimulation, indicating lack of effect on the muscarinic receptor and Gi protein. These results suggest that NIP-142 directly inhibits the acetylcholine-activated potassium current.
- 社団法人 日本薬理学会の論文
- 2006-08-20
著者
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Ito M
Meijo Univ. Nagoya Jpn
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Iida Tanaka
Department Of Food Science Otsuma Women's University
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Ito M
Graduate School Of Pharmaceutical Sciences Kyoto University
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Ito M
Department Of Pharmacognosy Graduate School Of Pharmaceutical Sciences Kyoto University
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Ito Michiho
北里大学 薬学部
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TANAKA Hikaru
Department of Pharmacology, Toho University School of
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SHIGENOBU Koki
Department of Pharmacology, Toho University School of
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Tanaka Hikaru
Dep. Of Pharmacology Toho Univ. Fac. Of Pharmaceutical Sciences Jpn
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Tanaka H
Department Of Pharmacology Toho University School Of Pharmaceutical Sciences
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Shigenobu K
Department Of Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Shigenobu K
Department Of Pharmacology Toho University School Of Pharmaceutical Sciences
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Shigenobu Koki
Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences The University Of Tokyo
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Tsuruoka Noriko
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Toho University
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Matsuda Tomoyuki
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Toho University
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ITO Mie
Department of Pharmacology, Toho University School of Pharmaceutical Sciences
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SAITO Tomoaki
Department of Pharmacology, Toho University School of Pharmaceutical Sciences
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YAMASHITA Toru
Biological Research Laboratories, Nissan Chemical Industries, Ltd.
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TSURUZOE Nobutomo
Biological Research Laboratories, Nissan Chemical Industries, Ltd.
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Tanaka Hikaru
Dep. Of Pharmacology Fac. Of Pharmaceutical Sciences Toho Univ.
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Tanaka Hikaru
Department Of Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Shigenobu Koki
Toho University School Of Pharmaceutical Sciences
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HASHIMOTO Norio
Biological Research Laboratories, Nissan Chemical Industries
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Ito Mie
Department Of Applied Biological Chemistry Graduate School Of Agricultural And Life Sciences Univers
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Iida Tanaka
Department Of Food Science Faculty Of Home Economics Otsuma Woman's University
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Saito Tomoaki
Department Of Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Yamashita Toru
Biological Research Laboratories Nissan Chemical Industries Ltd.
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ISHIMARU Sayoko
Department of Pharmacology, Toho University Faculty of Pharmaceutical Sciences
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Hashimoto Norio
Biological Research Laboratories Nissan Chemical Industries
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Hashimoto Norio
Biological Research Laboratories Nissan Chemical Industries Ltd.
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Ishimaru Sayoko
Department Of Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Tanaka Hikaru
Department Of Internal Medicine Sasebo Senjyu Hospital
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Yamashita Toru
Biological Research Laboratories Nissan Chemical Industries
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Matsuda Tomoyuki
Department Of Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Matsuda Tomoyuki
Department Of Anesthesiology And Anatomy And Neurobiology Kyoto Prefectural University Of Medicine
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Tanaka Hikaru
Department Of Internal Medicine Hirosaki Municipal Hospital
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Tanaka Hikaru
Department of Endocrinology and Metabolism, Hirosaki University
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TSURUOKA Noriko
Department of Pharmacology, Toho University Faculty of Pharmaceutical Sciences
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