心房細動治療薬のスクリーニング方法

Screening method of auricular fibrillation remedy

Abstract

【解決手段】▲1▼Naチャネルに対する試験物質の使用依存性抑制において、発現速度が0.3AP -1 以上であることを確認する工程及び▲2▼試験物質が、活性化状態のNaチャネルに対する高い親和性を有することを確認する工程、を含むことを特徴とする、活性化状態のNaチャネルに結合して、不活性化状態または静止状態のNaチャネルから速やかに解離する物質のスクリーニング方法,及び該方法によって特定される物質を含有する心房細動抑制剤並びにNaチャネル阻害剤。 【効果】 心房細動抑制剤等に使用できる物質を容易に判別できる。 【選択図】 なし
<P>PROBLEM TO BE SOLVED: To provide a material bonded to a Na-channel in cardiac muscle and having a blocking function only at the high-frequency pulsation time, especially a material exerting no influence on normal cardiac muscle activity, causing no arrhythmic interaction, excellent in safety and useful for auricular fibrillation treatment. <P>SOLUTION: This screening method of a material bonded to the Na-channel in the activated state and dissociated quickly from the Na-channel in the activated state or in the static state is characterized by including (1) a process for confirming that manifestation speed is 0.3 AP<SP>-1</SP>or more in use dependency suppression of a test material to the Na-channel, and (2) a process for confirming that the test material has high affinity to the Na-channel in the activated state. An auricular fibrillation depressant including the material specified by the method, and an Na-channel inhibitor are also provided. <P>COPYRIGHT: (C)2005,JPO&NCIPI

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    WO-2007023775-A1March 01, 2007Astellas Pharma Inc.心房細動治療剤