[Effect of phenazepam metabolite, 2-amino-5-bromo-2'-chlorobenzophenone, on glycine and glutamate NMDA receptors of rat hippocampal pyramidal neurones].
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.
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A.A. Bogomoletz Institute of Physiology, National Academy of Sciences of Ukraine, Kiev.
D000818:Animals; D014151:Anti-Anxiety Agents / Q000378:metabolism* / Q000494:pharmacology; D001569:Benzodiazepines; D001577:Benzophenones / Q000494:pharmacology*; D005071:Evoked Potentials / Q000187:drug effects* / Q000502:physiology; D006624:Hippocampus / Q000502:physiology; D066298:In Vitro Techniques; D009474:Neurons / Q000502:physiology; D018408:Patch-Clamp Techniques; D017966:Pyramidal Cells / Q000378:metabolism* / Q000502:physiology; D051381:Rats; D018009:Receptors, Glycine / Q000378:metabolism*; D016194:Receptors, N-Methyl-D-Aspartate / Q000378:metabolism*
C475862:2-amino-5-bromo-2'-chlorobenzophenone; D014151:Anti-Anxiety Agents; D001577:Benzophenones; D018009:Receptors, Glycine; D016194:Receptors, N-Methyl-D-Aspartate; D001569:Benzodiazepines; C017928:phenazepam