Anticonvulsant action of GBR-12909 and citalopram against acute experimentally induced limbic seizures

Neuropharmacology. 2004 Dec;47(7):1053-61. doi: 10.1016/j.neuropharm.2004.07.032.

Abstract

We recently showed that intrahippocampally administered dopamine and serotonin exert concentration-dependent non-protective, protective and proconvulsant effects against limbic seizures in rats. Anticonvulsant action was mediated via, respectively, hippocampal D2 and 5-HT1A receptor stimulation, while proconvulsant effects were associated with concomitant hippocampal glutamate increases. We here examined whether increases in endogenous hippocampal dopamine and serotonin exert similar actions. Initially, dose-response experiments were performed with intrahippocampal perfusions of GBR-12909 and citalopram, respectively, selective dopamine and serotonin re-uptake blockers. Based on their effects on monoaminergic release, a potential non-protective, protective and proconvulsant concentration was selected. The predicted non-protective GBR-12909 (10 microM) and citalopram (0.5 microM) concentrations failed to prevent pilocarpine-induced seizures. The predicted protective GBR-12909 (100 microM) and citalopram (1 microM) perfusions resulted in complete anticonvulsant action, again mediated by D2 and 5-HT1A receptors. Unexpectedly, at predicted proconvulsant concentrations complete anticonvulsant action was obtained and hippocampal Glu remained unaltered. This study shows that selective monoamine re-uptake blockers have important anticonvulsant properties. Based on the previously established anticonvulsant monoamine ranges, anticonvulsant threshold concentrations can be predicted for compounds with endogenous dopamine or serotonin promoting effects. Non-selective actions curtailing glutamatergic activity may further be responsible for the unexpected anticonvulsant effects at predicted proconvulsant concentrations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acute Disease
  • Animals
  • Anticonvulsants*
  • Biogenic Monoamines / metabolism
  • Citalopram / pharmacology*
  • Dopamine / metabolism
  • Dopamine Antagonists / pharmacology
  • Dopamine Uptake Inhibitors / pharmacology*
  • Dose-Response Relationship, Drug
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • Hippocampus / physiology
  • Limbic System / physiopathology*
  • Male
  • Microdialysis
  • Muscarinic Agonists / pharmacology
  • Pilocarpine / pharmacology
  • Piperazines / pharmacology*
  • Pyridines / pharmacology
  • Rats
  • Rats, Wistar
  • Remoxipride / pharmacology
  • Seizures / prevention & control*
  • Selective Serotonin Reuptake Inhibitors / pharmacology*
  • Serotonin / metabolism
  • Serotonin Antagonists / pharmacology

Substances

  • Anticonvulsants
  • Biogenic Monoamines
  • Dopamine Antagonists
  • Dopamine Uptake Inhibitors
  • Muscarinic Agonists
  • Piperazines
  • Pyridines
  • Serotonin Antagonists
  • Serotonin Uptake Inhibitors
  • Pilocarpine
  • Remoxipride
  • Citalopram
  • Serotonin
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide
  • vanoxerine
  • Dopamine