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

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.

authors

Danzin C,Collard JN,Marchal P,Schirlin D

doi

10.1016/0006-291x(89)92466-2

subject

Has Abstract

pub_date

1989-04-28 00:00:00

pages

540-4

issue

2

eissn

0006-291X

issn

1090-2104

pii

0006-291X(89)92466-2

journal_volume

160

pub_type

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