GABA receptors in clonal cell lines: a model for study of benzodiazepine action at molecular level

Science. 1979 Aug 24;205(4408):821-3. doi: 10.1126/science.462192.

Abstract

A "recptor unit" for gamma-aminobutyric acid (GABA), which includes brainlike receptor binding sites for tritium-labeled GABA and benzodiazepines (diazepam, clonazepam, and flunitrazepam) and a thermostable endogenous protein (GABA modulin) that inhibits both GABA and benzodiazepine binding, has been demonstrated in membranes prepared from NB2a neuroblastoma and C6 glioma clonal cell lines. In these cells, as in brain, diazepam (1 micromolar) prevents the effect of GABA modulin, and in turn GABA (0.oma and, to a lesser extent, the glioma cells represent a suitable model to study the interactions and the sequence of membrane and intracellular events triggered by the stimulation of benzodiazepine and GABA receptors.

MeSH terms

  • Animals
  • Benzodiazepines / metabolism*
  • Brain / metabolism*
  • Cell Line
  • Clonazepam / metabolism
  • Clone Cells / metabolism
  • Diazepam / metabolism
  • Diazepam / pharmacology
  • Flunitrazepam / metabolism
  • Membrane Proteins / pharmacology
  • Mice
  • Nerve Tissue Proteins / pharmacology
  • Rats
  • Receptors, Drug / metabolism*
  • gamma-Aminobutyric Acid / metabolism*

Substances

  • Membrane Proteins
  • Nerve Tissue Proteins
  • Receptors, Drug
  • Benzodiazepines
  • gamma-Aminobutyric Acid
  • Clonazepam
  • Flunitrazepam
  • Diazepam