Abstract：
:The specific binding of 35S-t-butylbicyclophosphorothionate (TBPS) was studied in synaptosomal membranes of rat cerebral cortex. The displacing potencies of eleven CNS depressants and three convulsants were determined in the presence of 1 microM GABA and 10 nM R 5135. GABA enhanced the displacing potencies of depressants of most diverse chemical structures: diaryltriazine (LY 81067), pyrazolopyridine (etazolate), cinnamide, glutarimide, 2,3-benzodiazepine (tofizopam) and alcohol derivatives, barbiturates, (+)etomidate, methaqualone and meprobamate. In contrast, the IC50 values of convulsants (picrotoxinin, pentetrazol and the barbiturate enantiomer S(+) MPPB) were not significantly affected. The depressants accelerated either basal or GABA-augmented dissociation of 35-TBPS mainly by increasing the contribution of its rapid first phase.
journal_name
Life Scijournal_title
Life sciencesauthors
Maksay G,Ticku MKdoi
10.1016/0024-3205(88)90589-9subject
Has Abstractpub_date
1988-01-01 00:00:00pages
1331-7issue
16eissn
0024-3205issn
1879-0631pii
0024-3205(88)90589-9journal_volume
43pub_type
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