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[Investigation of the anti-motion sickness effect of 3-hydroxypyridine derivatives].

Abstract
Experiments with rats showed that three out of 12 3-hydroxypyridine derivatives (ethyl-methyl hyd- roxypyrine succinate, SK-132 and IBCP-2 - had an anti-motion sickness effect stronger than of scopolamine, the reference vestiboloprotector. The anti-motion sickness effect of ethyl-methyl hydroxypyrine was also demonstrated in experiments with cats. Apparent anti-motion sickness effect of ethyl-methyl hydroxypyrine (mexydol) was found in 69% of healthy male volunteers which is comparable with the effect of scopolamine (62%). In experiments with immobilized cats (myorelaxation drugs) the microelectrode technique and microontoiphoresis of physiologically active substances revealed that ethylmethyl hydroxypyrine influences the majority of neurons in the medial vestibular nucleus (61%). Suppression of cell spontaneous activities in more than one half of cases can be stopped completely or attenuated significantly by bicucculine, a specific GABA(A)-receptor antagonist. In 42% of neurons ethyl-methyl hydroxypyrine subdues the response to vestibular stimulation which is likely to underlie the anti-motion sickness effect.
AuthorsV V Iasnetsov, V A Pravdivtsev, A V Shashkov, L D Smirnov, V V Iasnetsov, S B Kozlov, Iu V Ivanov
JournalAviakosmicheskaia i ekologicheskaia meditsina = Aerospace and environmental medicine (Aviakosm Ekolog Med) 2005 Jul-Aug Vol. 39 Issue 4 Pg. 45-50 ISSN: 0233-528X [Print] Russia (Federation)
PMID16353627 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • GABA Antagonists
  • Muscarinic Antagonists
  • Scopolamine
  • Bicuculline
Topics
  • Animals
  • Bicuculline (therapeutic use)
  • Cats
  • Disease Models, Animal
  • GABA Antagonists (therapeutic use)
  • Humans
  • Male
  • Motion Sickness (drug therapy, physiopathology)
  • Muscarinic Antagonists (therapeutic use)
  • Rats
  • Rats, Wistar
  • Scopolamine (therapeutic use)
  • Treatment Outcome
  • Vestibule, Labyrinth (drug effects, physiopathology)

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