Investigation of the anti-motion sickness effect of 3-hydroxypyridine derivatives
Iasnetsov, V.V.; Pravdivtsev, V.A.; Shashkov, A.V.; Smirnov, L.D.; Iasnetsov, V.V.; Kozlov, S.B.; Ivanov, I.V.
Aviakosmicheskaia i Ekologicheskaia Meditsina 39(4): 45-50
2005
ISSN/ISBN: 0233-528X PMID: 16353627 Document Number: 593100
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.