[Investigation of the anti-motion sickness effect of 3-hydroxypyridine derivatives].
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.
Iasnetsov
V V
VV
Pravdivtsev
V A
VA
Shashkov
A V
AV
Smirnov
L D
LD
Iasnetsov
V V
VV
Kozlov
S B
SB
Ivanov
Iu V
IuV
D000818:Animals; D001640:Bicuculline / Q000627:therapeutic use*; D002415:Cats; D004195:Disease Models, Animal; D018756:GABA Antagonists / Q000627:therapeutic use*; D006801:Humans; D008297:Male; D009041:Motion Sickness / Q000188:drug therapy* / Q000503:physiopathology; D018727:Muscarinic Antagonists / Q000627:therapeutic use; D051381:Rats; D017208:Rats, Wistar; D012601:Scopolamine / Q000627:therapeutic use*; D016896:Treatment Outcome; D014722:Vestibule, Labyrinth / Q000187:drug effects / Q000503:physiopathology
D018756:GABA Antagonists; D018727:Muscarinic Antagonists; D012601:Scopolamine; D001640:Bicuculline