Functional Proteins Involved in Regulation of Intracellular Ca^<2+> for Drug Development : Pharmacology of SEA0400, a Specific Inhibitor of the Na^+-Ca^<2+> Exchanger

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概要

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• The Na+-Ca2+ exchanger (NCX) is involved in regulation of intracellular Ca2+ concentration. A specific inhibitor of NCX has been required for clarification of the physiological and pathological roles of NCX. We have developed 2-[4-[(2,5-difluorophenyl)methoxy] phenoxy]-5-ethoxyaniline (SEA0400), a highly potent and selective inhibitor of NCX. SEA0400 in the concentration range that inhibits NCX exhibits negligible affinities for the Ca2+ channels, Na+ channels, K+ channels, noradrenaline transporter, and 14 receptors; and it does not affect the activities of the store-operated Ca2+ channel, Na+-H+ exchanger, and several enzymes including Na+,K+-ATPase and Ca2+-ATPase. Furthermore, recent studies show that SEA0400 attenuates ischemia-reperfusion injury in the brain, heart, and kidney and radiofrequency lesion-induced edema in rat brain. These findings suggest that NCX plays a key role in ischemia-reperfusion injury and may be a target molecule for treatment of reperfusion injury-related diseases.

• 社団法人 日本薬理学会の論文
• 2005-03-20

著者

• BABA Akemichi

  Laboratory of Molecular Neuropharmacology, Graduate School of Pharmaceutical Sciences, Osaka Univers

• Baba A

  Laboratory Of Molecular Neuropharmacology Graduate School Of Pharmaceutical Sciences Osaka Universit

• Baba Akemichi

  Lab. Of Veterinary Pharmacology Graduate School Of Life And Environmental Sci. Osaka Prefecture Univ

• Baba A

  Laboratory Of Molecular Neuropharmacology

• Baba Akemichi

  Laboratory Of Molecular Neuropharmacology Graduate School Of Pharmaceutical Sciences Osaka Universit

• Baba Akemichi

  昭和大学藤が丘病院 循環器内科

• Baba A

  昭和大学藤が丘病院 循環器内科

• Baba A

  Osaka Univ. Osaka Jpn

• Baba Akemichi

  サントリー生物医学研究所

• Matsuda T

  Lab. Of Medicinal Pharmacology Graduate School Of Pharmaceutical Sciences Osaka Univ.

• MATSUDA Toshio

  Laboratory of Medicinal Pharmacology, Graduate School of Pharmaceutical Sciences, Osaka University

• KOYAMA Yutaka

  Laboratory of Medicinal Pharmacology, Graduate School of Pharmaceutical Sciences, Osaka University

• Koyama Yutaka

  Laboratory Of Medicinal Pharmacology Graduate School Of Pharmaceutical Sciences Osaka University

• Matsuda Toshio

  Laboratory Of Medicinal Pharmacology Graduate School Of Pharmaceutical Sciences Osaka University

• Baba Akemichi

  Laboratory Of Molecular Neuropharmacology

• Baba Akemichi

  Laboratory Of Molecular Neuropharmacology Graduate School Of Pharmaceutical Sciences Osaka Universit

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