Selective inactivation of MAO-B by benzyl-dimethyl-silyl-methanamines in vitro |
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| Authors: | C Danzin J N Collard P Marchal D Schirlin |
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| Affiliation: | Merrell Dow Research Institute, Strasbourg, France. |
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| 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. |
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