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Stylbasole analogues of MPTP as monoamine oxidase (MAO) substrates

  • S. O. Sablin
  • S. O. Bachurin
  • S. E. Tkachenko
Conference paper
Part of the Journal of Neural Transmission book series (NEURAL SUPPL, volume 32)

Summary

Stylbasole analogs of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) were studied as monoamine oxidase (MAO) substrates. Dehydrogenation of these compounds was shown to be catalyzed by both serotonine specifical and benzylamine specifical MAO activities. Markedly high affinity of stylbasoles to B type of MAO was found. Influence of substrate structure on its biotransformation effectiveness is realized by the principle — “better binding-worse catalysis”. MAO inactivation during the reaction is appeared to be realized as result of product inhibition and perhaps of substrate inhibition.

Keywords

Monoamine Oxidase Enzyme Inactivation Affinity Center Inactivation Mechanism Dopaminergic Neurotoxicity 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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References

  1. Bachurin SO, Sablin SO, Grishina GV, Gaydarova EL, Dubova LG, Zubov ND (1989) Monoamine oxidase catalysis of bioconversion of physiologically active 1-methyl-4-aryl-1,2,3,6-tetrahydropyridines. Bioorganicheskaya khimia 15:620–626 (russ).Google Scholar
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  3. Heikkilla RE, Manzino L, Cabbat FS, Duvoisin RC (1984) Protection against the dopaminergic neurotoxicity of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine by monoamine oxidase inhibitors. Nature 311:467–469.CrossRefGoogle Scholar

Copyright information

© Springer-Verlag 1990

Authors and Affiliations

  • S. O. Sablin
    • 1
  • S. O. Bachurin
    • 1
  • S. E. Tkachenko
    • 1
  1. 1.Institute of Physiologically Active SubstancesAcademy of Sciences of USSRChernogolovka, Moscow RegionUSSR

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