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Inhibition of Monoamine Oxidase A-Form and Semicarbazide-Sensitive Amine Oxidase by Selective and Reversible Monoamine Oxidase-A Inhibitors, Amiflamine and FLA 788(+)

 

作者: Fumio Morikawa,   Toshihiko Ueda,   Yuichiro Arai,   Hiroyasu Kinemuchi,  

 

期刊: Pharmacology  (Karger Available online 1986)
卷期: Volume 32, issue 1  

页码: 38-45

 

ISSN:0031-7012

 

年代: 1986

 

DOI:10.1159/000138150

 

出版商: S. Karger AG

 

关键词: Semicarbazide-sensitive amine oxidase;Monoamine oxidase;Amiflamine;FLA 788(+);Rat lung

 

数据来源: Karger

 

摘要:

In vitro studies demonstrated that two selective monoamine oxidase (MAO)-A inhibitors, amiflamine and FLA 788(+), have been shown to inhibit semicarbazide-sensitive amine oxidase (SSAO) in rat testis and lung homogenates in a concentration-dependent way. The inhibition was not greatly influenced by pretreatment of the preparations with either clorgyline (10–3 mol/l), l-deprenyl (10–3 mol/l) or SKF 525A (10–4 mol/l). The two compounds showed a time-dependent inhibition of SSAO, and for the initial phase of the inhibition, amiflamine is a competitive inhibitor with a Kislope of 135 μmol/l, but FLA 788(+) is a noncompe-titive inhibitor with a Ki value of 180 μmol/l. After preincubation for 60 min at 37 °C, however, inhibition by amiflamine was found to be essentially irreversible whereas that produced by FLA 788(+) was still noncompetitive and reversible. These two compounds also reversibly and competitively inhibited rat testis MAO-A with FLA 788(+) being much more selective towards this MAO (Kislope = 0.26 μmol/l for FLA 788(+) and 7 μmol/l for amiflamine, respectively). The present results indicate that both MAO-A-selective inhibitors also inhibit SSAO in vitro, but their properties as SSAO inhibitors differ from those as MAO-A

 

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