Hiroyasu Kinemuchi1, Masato Jinbo1, Atsushi Tabata1,
Yoshie Toyoshima2, Yuichiro Arai2,
Takeshi Tadano3, Kensuke Kisara3 and Lars Oreland4
1Laboratoryﾊof Enzyme Pharmacology, Senshu University at Ishinomaki,
Ishinomaki 986-8580, Japan
2Departmentﾊof Pharmacology, School of Medicine, Showa University,
Tokyo 142-8555, Japan
3Departmentﾊof Pharmacology, Tohoku Pharmaceutical University,
Sendai 981-8558, Japan
4Sectionﾊ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ﾊ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