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Selective inactivation of MAO-B by benzyl-dimethyl-silyl-methanamines in vitro.

作者信息

Danzin C, Collard J N, Marchal P, Schirlin D

机构信息

Merrell Dow Research Institute, Strasbourg, France.

出版信息

Biochem Biophys Res Commun. 1989 Apr 28;160(2):540-4. doi: 10.1016/0006-291x(89)92466-2.

DOI:10.1016/0006-291x(89)92466-2
PMID:2719680
Abstract

The alpha-silyl amines benzyl-dimethyl-silyl-methanamine and the p-fluoro and p-chloro derivatives are potent time-dependent inhibitors of rat brain MAO-B. The inhibition exhibits saturation kinetics, takes place in the enzyme active-site and is irreversible. The most potent inhibitor in the series is 4-fluorobenzyl-dimethyl-silyl-methanamine (KI = 11 microM, tau 1/2 = 2.3 min). Its selectivity for the B-form relative to the A-form of rat brain MAO is higher than 10(4). Benzyl-dimethyl-silyl-methanamines may represent a new family of anti-Parkinsonian agents.

摘要

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