[Effect of multiple daily administration of fenibut and diazepam on GABA and benzodiazepine receptors in the mouse brain].
It was shown in experiments on mice that 25 hours after chronic treatment with fenibut (100 mg/kg, twice daily for 10 days) was discontinued the number of benzodiazepine and GABAA (bicucullin-sensitive) receptor sites was increased and 48 hours after treatment discontinuation the number of GABAB (bicucullin nonsensitive) sites was decreased. The enhanced binding to GABAA and GABAB receptor sites and the decreased binding to benzodiazepine receptors was observed 24 hours after discontinuation of chronic treatment with diazepam (5 mg/kg, twice daily). Forty-eight hours after diazepam chronic treatment was discontinued the number of benzodiazepine receptor sites was increased. The involvement of the increased benzodiazepine receptor sensitivity in the mechanism of therapeutic activity of fenibut is suggested.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000378:metabolism*; D001640:Bicuculline / Q000494:pharmacology; D001921:Brain / Q000187:drug effects*; D003975:Diazepam / Q000008:administration & dosage*; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D011955:Receptors, Drug / Q000187:drug effects*; D017981:Receptors, Neurotransmitter / Q000187:drug effects*; D005680:gamma-Aminobutyric Acid / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism*
D014151:Anti-Anxiety Agents; D011955:Receptors, Drug; D017981:Receptors, Neurotransmitter; D005680:gamma-Aminobutyric Acid; D003975:Diazepam; C008842:4-amino-3-phenylbutyric acid; D001640:Bicuculline
Vliianie mnogodnevnogo vvedeniia fenibuta i diazepama na retseptory GAMK i benzodiazepinov v mozge mysheĭ.