Novel Monoamine Oxidase Inhibitors, 3-(2-Aminoethoxy)-1,2-benzisoxazole Derivatives, and Their Differential Reversibility
スポンサーリンク
概要
- 論文の詳細を見る
Although possible usefulness of non-selective monoamine oxidase (MAO) inhibitors for Parkinson’s disease therapy has been suggested in the literature, MAO inhibitors whose inhibition is reversible and have dual action to both MAO-A and -B subtypes is not available yet. Subtype selectivity and reversibility of a series of novel MAO inhibitors, 3-(2-aminoethoxy)-1,2-benzisoxazole derivatives, were studied. Several dual MAO inhibitors, which inhibit both MAO-A and -B, were obtained. When administered to mice, their effects were generally reversible. Among the derivatives, RS-1636 and RS-1653 had much longer duration of brain MAO-B inhibition than that of MAO-A. In vitro, the inhibited MAO-A activity by these compounds was partially recovered by buffer change at 4°C, while little MAO-B activity was recovered. Although it is not fully elucidated yet, the reversibility of these inhibitors is probably determined primarily by this dissociation profile. This unique differential reversibility indicates that optimization of the balance of actions can be achieved by differentiating reversibility to each target molecule.
- 社団法人 日本薬理学会の論文
- 2002-02-01
著者
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KOZUKA Masao
Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd.
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Kozuka Masao
Neuroscience And Immunology Research Laboratories Sankyo Co. Ltd
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Iwata N
Science Information Co. Ltd
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Kojima Kouichi
Institute Of Science And Technology Inc
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YOSHIMI Kenji
Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd
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SAKAI Jyunichi
Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd
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IIZAWA Tomoko
Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd
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SHIMIZU Yuki
Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd
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KANEKO Isao
Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd
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IWATA Nobuyoshi
Science Information Co., Ltd
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Yoshimi Kenji
Neuroscience And Immunology Research Laboratories Sankyo Co. Ltd
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Kaneko Isao
Neuroscience And Immunology Research Laboratories Sankyo Co. Ltd
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Iizawa Tomoko
Neuroscience And Immunology Research Laboratories Sankyo Co. Ltd
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Sakai J
Neuroscience And Immunology Research Laboratories Sankyo Co. Ltd
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Shimizu Yuki
Neuroscience And Immunology Research Laboratories Sankyo Co. Ltd
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Sakai Jyunichi
Neuroscience And Immunology Research Laboratories Sankyo Co. Ltd
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