CNS depressants accelerate the dissociation of 35S-TBPS binding and GABA enhances their displacing potencies

G. Maksay, M. K. Ticku

Research output: Contribution to journalArticlepeer-review

12 Scopus citations

Abstract

The specific binding of 35S-t-butylbicyclophos-phorothionate (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 μM 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.

Original languageEnglish (US)
Pages (from-to)1331-1337
Number of pages7
JournalLife Sciences
Volume43
Issue number16
DOIs
StatePublished - 1988

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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