Characterization of the Pharmacology of YM-198313 on Volume-Regulated Anion Channels(Pharmacology)
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概要
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Activation of the volume-regulated anion channels (VRAC) is considered to be involved in arrhythmia, but it has not yet been fully elucidated because of the lack of its high affinitive and selective compounds. A newly synthesized compound, YM-198313 (sodium 4-({[2-(methylthio)benzyl]amino}-5-[(1-phenylethyl)thio]isothiazol-3-olate), strongly inhibited VRAC in HeLa cells with an IC_<50> of 3.03±0.05μM. However, YM-198313 weakly affected both the Ca^<2+>-activated Cl^- channels in HTC cells and the cAMP-activated Cl^- channels in T84 cells, demonstrating that this compound is selective for VRAC among Cl^- channels. At 10μM, YM-198313 almost completely (100±7.8%) inhibited the VRAC current in guinea pig atrial myocytes. However, at the same concentration, YM-198313 showed little inhibitory effect on the cardiac cation currents in ventricular myocytes. We believe that YM-198313 is a potent and selective VRAC inhibitor, therefore, it should be use to clarify the role VRAC plays in arrhythmia.
- 2005-07-01
著者
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SHIBATA Hiroshi
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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SATOH Tomo
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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UGAWA Tohru
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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MASUDA Noriyuki
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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INAMURA Hiroko
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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ABE Asaki
Department of Animal Science and Technology, Okayama University Graduate School of Natural Science a
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KONDO Yasuhiro
Department of Animal Science and Technology, Okayama University Graduate School of Natural Science a
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KURAMOCHI Takahiro
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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AKAMATSU Seijiro
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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UCHIDA Wataru
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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Abe Asaki
中華人民共和国
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Abe Asaki
Department Of Animal Science And Technology Faculty Of Agriculture Okayama University
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Satoh Tomo
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco
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Ugawa Tohru
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Ugawa Tohru
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco
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Uchida Wataru
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Uchida Wataru
山之内製薬
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Kondo Yasuhiro
中華人民共和国
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Inamura Hiroko
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco
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Masuda Noriyuki
筑波大学 人間総合科学研究科循環器病態医学
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Masuda Noriyuki
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.
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Akamatsu Seijiro
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco
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Kuramochi Takahiro
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco
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Shibata Hiroshi
Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:department Of Animal Scienc
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Kondo Yasuhiro
Department Of Animal Science And Technology Okayama University Graduate School Of Natural Science An
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Satoh Tomo-Oki
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.
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SHIBATA Hiroshi
Institute for Biomedical Research, Suntory Limited
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