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

• Published in: Japanese Journal of Pharmacology Vol. 83; no. 2; pp. 164 - 166
• Main Authors: Kinemuchi, Hiroyasu, Jinbo, Masato, Tabata, Atsushi, Toyoshima, Yoshie, Arai, Yuichiro, Tadano, Takeshi, Kisara, Kensuke, Oreland, Lars
• Format: Journal Article
• Language: English
• Published: Japan The Japanese Pharmacological Society 2000
• Subjects: 2-Bromoethylamine (2-BEA); Amine Oxidase (Copper-Containing) - antagonists & inhibitors; Animals; Enzyme Inhibitors - pharmacology; Ethylamines - pharmacology; Kinetics; Male; Rats; Rats, Sprague-Dawley; Semicarbazide-sensitive amine oxidase (SSAO); Suicide inhibitor; Semicarbazide-sensitive amine oxidase (SSAO); 2-Bromoethylamine (2-BEA); Suicide inhibitor
• ISSN: 0021-5198; 1347-3506
• DOI: 10.1016/S0021-5198(19)30614-6

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 μM. 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.