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The influence of the antidepressant pirlindole and its dehydro-derivative on the activity of monoamine oxidase A and GABAA receptor binding

  • A. E. Medvedev
  • V. I. Shvedov
  • T. M.
  • O. A. Fedotova
  • E. Saederup
  • R. F. Squires
Part of the Journal of Neural Transmission. Supplement book series (NEURAL SUPPL, volume 52)

Summary

The influence of pirlindole and dehydro-pirlindole on GABAA receptor binding and MAO-A activity was investigated in vitro. Inhibition of rat brain and human placenta MAO-A by both compounds was much more potent (with IC50 range 0.3–0.005 μM) than that of GABAA receptors. Pirlindole was inactive as a GABA antagonist. Dehydro-pirlindole exhibited selective blockade of GAB A-A receptors with EC50 12 μM. Effects of both compounds on MAO-A activity were partially reversible. Data obtained suggest that in contrast to pirlindole dehydro-pirlindole may act not only as a MAO-A inhibitor but also as a potent GABAA receptor blocker.

Keywords

GABAA Receptor Monoamine Oxidase Biomedical Chemistry Gaba Antagonist TBPS Binding 
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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Copyright information

© Springer-Verlag Wien 1998

Authors and Affiliations

  • A. E. Medvedev
    • 1
    • 1
  • V. I. Shvedov
    • 2
  • T. M.
    • 1
  • O. A. Fedotova
    • 2
  • E. Saederup
    • 3
  • R. F. Squires
    • 3
  1. 1.Institute of Biomedical ChemistryAcademy of Medical SciencesMoscowRussia
  2. 2.Centre of Drug Chemistry — Institute of Pharmaceutical ChemistryMoscowRussia
  3. 3.Nathan Kline Institute for Psychiatric ResearchOrangeburgUSA

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