title: [A new approach to the search for vestibuloprotectors].
abstract: The results of experimental clinical testing of the antinaupathia action of as new compounds, so motion sickness medications (promethazine, ikaron-1 etc.) are presented. Russian medication mexidol, a derivative of 3-hydroxypyridine (3-HP) demonstrated the ability to control motion sickness in humans and animals; however, unlike reference vestibuloprotector scopolamine, it does not practically produce side-effects. Mexidol acts through ion pathways with the involvement of glutamate and GABA-ergic components. Revealed 9 of new 3-HP derivates with an antimotion sickness effect in rats, three exceeded in efficacy mexidol, and also reference medications (i.e. scopolamine and promethazine). Melatonin achieves a better vestiboloprotective effect in rats than promethazine and melatonin-ergic antidepressant agomelatine through the involvement of melatonin MT1-, MT2- and GABA(A)-receptors. Also, combinations of melatonin with mexidol or promethazine possess a distinct vestibuloprotective effect, as melatonin enhances the action of equally mexidol and promethazine. Analysis of our results and investigations of other authors infer that search for potent vestibuloprotectors should be extended to new 3-HP derivatives and melatoninergic compounds. Individual medications by themselves and in combinations can become a solution to the problem.
authors.forename: V V
authors.initials: VV
authors.lastname: Yasnetsov
authors.forename: S K
authors.initials: SK
authors.lastname: Karsanova
authors.forename: Vic V
authors.initials: VV
authors.lastname: Yasnetsov
mesh_terms: D000081:Acetamides / Q000494:pharmacology; D000818:Animals; D015195:Drug Design; D018698:Glutamic Acid / Q000378:metabolism; D006801:Humans; D008550:Melatonin / Q000378:metabolism / Q000494:pharmacology; D009041:Motion Sickness / Q000188:drug therapy*; D010847:Picolines / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use*; D011398:Promethazine / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D051381:Rats; D011963:Receptors, GABA-A / Q000378:metabolism; D044094:Receptors, Melatonin / Q000378:metabolism; D012601:Scopolamine / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D009281:Naphthalenes
chemical_list: D000081:Acetamides; D018698:Glutamic Acid; D008550:Melatonin; D010847:Picolines; D011398:Promethazine; D011963:Receptors, GABA-A; D044094:Receptors, Melatonin; D012601:Scopolamine; C084711:agomelatine; D009281:Naphthalenes; C070020:emoxypine succinate