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(R)(+)-N-炔丙基-1-氨基茚(雷沙吉兰)及其衍生物:单胺氧化酶B的高选择性强效抑制剂。

(R)(+)-N-propargyl-1-aminoindan (rasagiline) and derivatives: highly selective and potent inhibitors of monoamine oxidase B.

作者信息

Sterling J, Veinberg A, Lerner D, Goldenberg W, Levy R, Youdim M, Finberg J

机构信息

Teva Pharmaceutical Industries, Jerusalem, Israel.

出版信息

J Neural Transm Suppl. 1998;52:301-5. doi: 10.1007/978-3-7091-6499-0_30.

Abstract

(+)-N-Propargyl-1-aminoindan (rasagiline) and a series of derivatives have been synthesized and screened for monoamine oxidase inhibitory activity. Rasagiline and several analogues were found be highly selective and potent inhibitors of the B form of the enzyme in contrast to the levorotatory enantiomer which was not active. The results indicate that rasagiline has potential for the treatment of Parkinson's Disease. This compound is currently under development for that indication.

摘要

(+)-N-炔丙基-1-氨基茚(雷沙吉兰)及其一系列衍生物已被合成并筛选其单胺氧化酶抑制活性。结果发现,与无活性的左旋对映体相比,雷沙吉兰和几种类似物是该酶B型的高度选择性和强效抑制剂。这些结果表明雷沙吉兰具有治疗帕金森病的潜力。该化合物目前正针对该适应症进行研发。

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