Effect of flumazenil on GABAA receptors in isolated rat hippocampal neurons |
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| Authors: | Weiss Michel Tikhonov Denis Buldakova Svetlana |
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| Institution: | (1) Laboratoire de physiopathologie et action thérapeutique des gaz sous pression, EA 3280, Université de la Méditerranée et IMNSSA, Faculté de Médecine Nord, I.F.R. Jean Roche, 13916 Marseille, cedex 20, France;(2) Laboratory of biophysic of synaptic processes, Sechenov Institute of Evolutionary Physiology and Biochemistry, Russian Academy of Sciences, Saint-Petersburg, Russia |
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| Abstract: | Using whole cell patch-clamp recordings from pyramidal cells acutely dissociated from rat hippocampal slices, Ro-15 1788 (flumazenil, FLU) was shown to enhance the GABAA-receptor mediated currents evoked by application of  -aminobutyric acid (GABA) and to antagonize the enhancing effect of the benzodiazepine agonist flurazepam (FZP) on the GABAA response. Both FLU and FZP increased the peak and the steady-state components of the responses and accelerated the current decay. This suggests that both agents act via a common mechanism on GABA transmission. It is concluded that FLU possesses high affinity for the binding site, but low efficacy on the GABAA-benzodiazepine receptor. This suggests that FLU acts as a partial agonist on GABAA receptors. |
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| Keywords: | Rat hippocampus pyramidal cells whole-cell patch-clamp GABAA receptors flumazenil flurazepam |
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