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

被引:13
|
作者
Kinemuchi, H [1 ]
Jinbo, M
Tabata, A
Toyoshima, Y
Arai, Y
Tadano, T
Kisara, K
Oreland, L
机构
[1] Ishinomaki Senshu Univ, Lab Enzyme Pharmacol, Ishinomaki 9868580, Japan
[2] Showa Univ, Sch Med, Dept Pharmacol, Tokyo 1428555, Japan
[3] Tohoku Pharmaceut Univ, Dept Pharmacol, Sendai, Miyagi 9818558, Japan
[4] Uppsala Univ, Ctr Biomed, Dept Neurosci, Pharmacol Sect, S-75124 Uppsala, Sweden
来源
JAPANESE JOURNAL OF PHARMACOLOGY | 2000年 / 83卷 / 02期
关键词
semicarbazide-sensitive amine oxidase (SSAO); 2-bromoethylamine (2-BEA); suicide inhibitor;
D O I
10.1254/jjp.83.164
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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 K-i value of 2.5 mu M. 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.
引用
收藏
页码:164 / 166
页数:3
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