2-溴乙胺，一种组织结合型氨基脲敏感胺氧化酶的自杀性抑制剂。

2-Bromoethylamine, a suicide inhibitor of tissue-bound semicarbazide-sensitive amine oxidase.

作者信息

Kinemuchi H, Jinbo M, Tabata A, Toyoshima Y, Arai Y, Tadano T, Kisara K, Oreland L

机构信息

Laboratory of Enzyme Pharmacology, Senshu University at Ishinomaki, Japan.

出版信息

Jpn J Pharmacol. 2000 Jun;83(2):164-6. doi: 10.1254/jjp.83.164.

DOI:10.1254/jjp.83.164

PMID:10928332

Abstract

Various mammalian tissues contain plasma membrane-bound amine oxidase, termed semicarbazide-sensitive amine oxidase (SSAO). In the present study, 2-bromoethylamine has been studied with regard to inhibitory properties towards tissue-bound SSAO in rat lung. Without preincubation, 2-bromoethylamine was a competitive and reversible SSAO inhibitor with a Ki value of 2.5 microM. After preincubation, it time-dependently and non-competitively inhibited SSAO activity, probably by forming the covalently-bound enzyme-inhibitor adduct. The data presented suggest that 2-bromoethylamine may act as a suicide inhibitor of SSAO.

摘要

多种哺乳动物组织含有与质膜结合的胺氧化酶，称为氨基脲敏感胺氧化酶（SSAO）。在本研究中，已对2-溴乙胺对大鼠肺组织中结合型SSAO的抑制特性进行了研究。在没有预温育的情况下，2-溴乙胺是一种竞争性、可逆的SSAO抑制剂，Ki值为2.5微摩尔。预温育后，它以时间依赖性和非竞争性方式抑制SSAO活性，可能是通过形成共价结合的酶-抑制剂加合物。所呈现的数据表明，2-溴乙胺可能作为SSAO的自杀性抑制剂起作用。