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

• SHIBATA Hiroshi

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• SATOH Tomo

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• UGAWA Tohru

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• MASUDA Noriyuki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• INAMURA Hiroko

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• ABE Asaki

  Department of Animal Science and Technology, Okayama University Graduate School of Natural Science a

• KONDO Yasuhiro

  Department of Animal Science and Technology, Okayama University Graduate School of Natural Science a

• KURAMOCHI Takahiro

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• AKAMATSU Seijiro

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• UCHIDA Wataru

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• Abe Asaki

  中華人民共和国

• Abe Asaki

  Department Of Animal Science And Technology Faculty Of Agriculture Okayama University

• Satoh Tomo

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco

• Ugawa Tohru

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Ugawa Tohru

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco

• Uchida Wataru

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Uchida Wataru

  山之内製薬

• Kondo Yasuhiro

  中華人民共和国

• Inamura Hiroko

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco

• Masuda Noriyuki

  筑波大学 人間総合科学研究科循環器病態医学

• Masuda Noriyuki

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.

• Akamatsu Seijiro

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco

• Kuramochi Takahiro

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:(present Address)drug Disco

• Shibata Hiroshi

  Institute For Drug Discovery Research Yamanouchi Pharmaceutical Co. Ltd.:department Of Animal Scienc

• Kondo Yasuhiro

  Department Of Animal Science And Technology Okayama University Graduate School Of Natural Science An

• Satoh Tomo-Oki

  Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd.

• SHIBATA Hiroshi

  Institute for Biomedical Research, Suntory Limited

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