RS-1636(RS-1636) - 药物靶点：MAO-A x MAO-B_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

MAO-A x MAO-B

作用机制

MAO-A抑制剂(单胺氧化酶A抑制剂)、MAO-B抑制剂(单胺氧化酶B抑制剂)

治疗领域

神经系统疾病内分泌与代谢疾病

在研适应症-

非在研适应症

帕金森病

原研机构

Sankyo Co., Ltd. (Tokyo)

在研机构-

非在研机构

Sankyo Co., Ltd. (Tokyo)

最高研发阶段无进展药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

关联

100 项与 RS-1636 相关的临床结果

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100 项与 RS-1636 相关的转化医学

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100 项与 RS-1636 相关的专利（医药）

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1

项与 RS-1636 相关的文献（医药）

2002-01-01·Japanese Journal of Pharmacology

Novel Monoamine Oxidase Inhibitors, 3-(2-Aminoethoxy)-1,2-benzisoxazole Derivatives, and Their Differential Reversibility

Article

作者: Kouichi Kojima ; Tomoko Iizawa ; Nobuyoshi Iwata ; Kenji Yoshimi ; Masao Kozuka ; Isao Kaneko ; Jyunichi Sakai ; Yuki Shimizu

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 degrees 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.

100 项与 RS-1636 相关的药物交易

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