Boyko I. The molecular mode of action of the hypnotic and anxiolytic agent cinazepam

The dissertation is devoted to study of cinazepam action neurochemical mechanism, his biotransformation both in vitro and in vivo, and bioavailability in its ?-cyclodextrines complex administration. It was determined that cinazepam is the partial agonist of CBDR with Кi 72 nМ, GS 1,3 cinazepams tolerance formation more slowly as compared to the zopiclon. It was demonstrated the GABAA-receptors complex functional states full regeneration after the prolonged administrations disrupting take place in 7 days. It was determined that prolonged cinazepam and zopiclon administration alter the studies rats head brain neuromediatory systems receptors activity, the most global changes investigate in dopaminergic system receptors case.It was demonstrated the possibility of cinazepam bioavailability and tissue (brain) ability increase in 2,4 and 2,9 as much, accordingly, after his peroral administration in complex with ?-cyclodextrine, cinazepam is biotransformed more quickly in brain than in blood plasma.