GABAA antagonists reveal binding sites for [35S]TBPS in cerebellar granular cell layer

Eur J Pharmacol. 1992 Feb 18;211(3):427-8. doi: 10.1016/0014-2999(92)90402-p.

Abstract

Autoradiography revealed picrotoxin-sensitive [35S]TBPS ([35S]t-butylbicyclophosphorothionate) binding sites in the cerebellar granule cell layer only in the presence of GABAA receptor antagonists. However, under the same conditions, the binding was decreased in other brain regions, including the cerebellar molecular cell layer. Thus, the convulsant binding sites at GABAA receptors in the granule cell layer are highly sensitive to down-regulation by GABA, which may be due to a unique combination of receptor subunits.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Androstanes / pharmacology
  • Animals
  • Autoradiography
  • Azasteroids / pharmacology
  • Binding Sites
  • Brain / metabolism
  • Brain / ultrastructure
  • Bridged Bicyclo Compounds / metabolism*
  • Bridged Bicyclo Compounds, Heterocyclic*
  • Cerebellar Cortex / cytology
  • Cerebellar Cortex / metabolism
  • Cerebellar Cortex / ultrastructure*
  • Convulsants / metabolism
  • GABA Antagonists
  • GABA-A Receptor Antagonists*
  • Male
  • Pyridazines / pharmacology
  • Rats
  • Rats, Inbred Strains
  • Sulfur Radioisotopes

Substances

  • Androstanes
  • Azasteroids
  • Bridged Bicyclo Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Convulsants
  • GABA Antagonists
  • GABA-A Receptor Antagonists
  • Pyridazines
  • Sulfur Radioisotopes
  • tert-butylbicyclophosphorothionate
  • gabazine
  • RU 5135