[Effect of phenazepam metabolite, 2-amino-5-bromo-2'-chlorobenzophenone, on glycine and glutamate NMDA receptors of rat hippocampal pyramidal neurones]

Fiziol Zh. 2003;49(1):23-7.
[Article in Ukrainian]

Abstract

Action of 2-amino-5-bromo-2'-chlorobenzophenone (ABPH), a metabolite of phenazepam, on currents evoked by the activation of glycine and glutamate NMDA receptors has been investigated in enzymatically isolated hippocampal rat pyramidal neurones. It is demonstrated that 3-10 microM ABPH caused an inhibitory effect on glycine receptors which was more prominent after pre-incubation with the drug. Peak amplitude of NMDA receptor-mediated currents was weakly potentiated after prolonged (4-6 min) incubation with 10 microM ABPH. Thus, the effects of the benzophenone metabolites should be taken into account when analysing the action of phenazepam and other benzodiazepine drugs.

Publication types

  • English Abstract

MeSH terms

  • Animals
  • Anti-Anxiety Agents / metabolism*
  • Anti-Anxiety Agents / pharmacology
  • Benzodiazepines*
  • Benzophenones / pharmacology*
  • Evoked Potentials / drug effects*
  • Evoked Potentials / physiology
  • Hippocampus / physiology
  • In Vitro Techniques
  • Neurons / physiology
  • Patch-Clamp Techniques
  • Pyramidal Cells / metabolism*
  • Pyramidal Cells / physiology
  • Rats
  • Receptors, Glycine / metabolism*
  • Receptors, N-Methyl-D-Aspartate / metabolism*

Substances

  • 2-amino-5-bromo-2'-chlorobenzophenone
  • Anti-Anxiety Agents
  • Benzophenones
  • Receptors, Glycine
  • Receptors, N-Methyl-D-Aspartate
  • Benzodiazepines
  • phenazepam