Jpn. J. Pharmacol. 83 (2), 164-166 (2000)


2-Bromoethylamine, a Suicide Inhibitor of Tissue-Bound Semicarbazide-Sensitive Amine Oxidase

Hiroyasu Kinemuchi1, Masato Jinbo1, Atsushi Tabata1, Yoshie Toyoshima2, Yuichiro Arai2,
Takeshi Tadano3, Kensuke Kisara3 and Lars Oreland4


1Laboratory╩of Enzyme Pharmacology, Senshu University at Ishinomaki, Ishinomaki 986-8580, Japan
2Department╩of Pharmacology, School of Medicine, Showa University, Tokyo 142-8555, Japan
3Department╩of Pharmacology, Tohoku Pharmaceutical University, Sendai 981-8558, Japan
4Section╩of Pharmacology, Department of Neuroscience, Box 593, Biomedical Centre, Uppsala University, Uppsala 751 24, Sweden

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╩mM. 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.

Keywords: Semicarbazide-sensitive amine oxidase (SSAO), 2-Bromoethylamine (2-BEA), Suicide inhibitor


Copyrightę The Japanese Pharmacological Society 2000

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