Benzodiazepine receptor: demonstration in the central nervous system

Science. 1977 Nov 25;198(4319):849-51. doi: 10.1126/science.918669.

Abstract

Diazepam, a potent minor tranquilizer, binds with high affinity to a specific benzodiazepine receptor that occurs exclusively in the central nervous system. The receptor is mainly localized in the synaptic membrane fraction. Binding to the receptor is stereospecific. Competition for the receptor by various benzodiazepines closely parallels their pharmacological potency.

MeSH terms

  • Animals
  • Benzodiazepines / metabolism*
  • Binding Sites
  • Brain / metabolism
  • Brain / ultrastructure*
  • Diazepam / metabolism
  • In Vitro Techniques
  • Molecular Conformation
  • Rats
  • Receptors, Drug / isolation & purification*
  • Receptors, Drug / metabolism
  • Stereoisomerism
  • Structure-Activity Relationship
  • Synaptic Membranes / metabolism*
  • Synaptosomes / metabolism
  • Tritium

Substances

  • Receptors, Drug
  • Tritium
  • Benzodiazepines
  • Diazepam